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Therapy Name | Imatinib |
Synonyms | |
Therapy Description |
Gleevec (imatinib) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (PMID: 12200353). Gleevec (imatinib) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Imatinib | Gleevec | CGP-57148B|STI571|Imatinib mesylate | ABL Inhibitor (pan) 9 BCR-ABL Inhibitor 32 CSF1R Inhibitor 28 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 | Gleevec (imatinib) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (PMID: 12200353). Gleevec (imatinib) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT M552_D572del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to partial responses in two patients with gastrointestinal stromal tumors harboring KIT M552_D572del, with a progression-free survival (PFS) of 25.2 mo and overall survival (OS) of 32 mo in one patient, and a PFS of 50.9 mo and OS of 53.9 mo in the second patient (PMID: 18294292). | 18294292 |
KIT V654A | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, cells expressing KIT V654A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 16751810). | 16751810 |
KIT E554_Y570del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumor harboring KIT E554_Y570del, with a progression-free survival of 11.5 months and overall survival of 34.1 months (PMID: 18294292). | 18294292 |
KIT positive | gastrointestinal stromal tumor | sensitive | Imatinib | FDA approved | Actionable | In a Phase II trial that supported FDA approval, treatment with Gleevec (imatinib) resulted in an overall response rate of 38% (56/147) and a median duration of response of 13 weeks in patients with metastatic or unresectable KIT-positive GIST (PMID: 12374669). | 12374669 detail... |
KIT K558_G565delinsR | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib) treatment resulted in tumor regression and decreased mitotic activity in gastrointestinal stromal tumor patient derived xenograft (PDX) models harboring KIT K558_G565delinsR (PMID: 27777285). | 27777285 |
KIT V569_L576del KIT V654A KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT V654A and KIT N822K were identified as secondary mutations in a patient with gastrointestinal stromal tumor harboring a primary KIT V569_L576del mutation, who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
CTNNB1 S45F | desmoid tumor | sensitive | Imatinib | Clinical Study - Cohort | Actionable | In a retrospective analysis, patients with desmoid fibromatosis harboring CTNNB1 S45F demonstrated a greater progression arrest rate at 6 months compared to CTNNB1 wild-type patients (85% vs 43%, p=0.05) when treated with Gleevec (imatinib) (PMID: 26861905). | 26861905 |
KIT A502_Y503dup | gastrointestinal stromal tumor | conflicting | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib) treatment stabilized tumor growth in a gastrointestinal stromal tumor patient-derived xenograft (PDX) model harboring KIT A502_Y503dup (PMID: 35625872). | 35625872 |
KIT A502_Y503dup | gastrointestinal stromal tumor | conflicting | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, a gastrointestinal stromal tumor patient-derived xenograft (PDX) model harboring KIT A502_Y503dup demonstrated resistance to treatment with Gleevec (imatinib), resulting in increased tumor volume (PMID: 27777285). | 27777285 |
KIT W557_K558del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in 4 partial responses and 1 stable disease in 5 patients with gastrointestinal stromal tumors harboring KIT W557_K558del, with progression-free survival ranging from 12.2 to 36.5 months and overall survival ranging from 22.7 to 67.9 months (PMID: 18294292). | 18294292 |
KIT V560_D572del KIT A829P | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT KIT V560_D572del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT A829P (PMID: 18294292). | 18294292 |
KIT V560D KIT D820A | gastrointestinal stromal tumor | resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT D820A was identified as a secondary mutation in a patient with gastrointestinal stromal tumor harboring a primary KIT V560D mutation, who developed resistance to Gleevec (imatinib mesylate) (PMID: 16954519). | 16954519 |
KIT V560D KIT D820A | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, a gastrointestinal stromal tumor cell line harboring KIT V560D and KIT D820A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 16954519). | 16954519 |
ABL1 T315I ABL1 R332W | lung adenocarcinoma | resistant | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, lung adenocarcinoma cells harboring ABL1 R332W (also reported as R351W) and expressing ABL1 T315I demonstrated resistance to Gleevec (imatinib) in culture and in xenograft models (PMID: 26758680). | 26758680 |
KIT V560G KIT D816V | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560G and D816V demonstrated resistance to Gleevec (imatinib) treatment in culture (PMID: 30523507). | 30523507 |
KIT A502_Y503dup KIT V654A | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT V654A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT Q556_W557del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT Q556_W557del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT V654A (PMID: 18294292). | 18294292 |
KIT W557G | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib mesylate) inhibited Kit phosphorylation efficiently in transformed human cells over expressing KIT W557G in culture (PMID: 23567324). | 23567324 |
FLT3 Y842C | acute myeloid leukemia | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, primary AML blasts expressing FLT3 Y842C were resistant to Gleevec (imatinib) as demonstrated by constitutively phosphorylated FLT3 and STAT-5 (PMID: 15345593). | 15345593 |
KIT V560G KIT D816V | mast cell neoplasm | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, mast cells harboring both KIT D816V and KIT V560G were resistant to Gleevec (imatinib) in culture (PMID: 31085175). | 31085175 |
KIT Q556_K558del | gastric adenocarcinoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in a partial response with tumor shrinkage lasting at least 1 year in a patient with metastatic gastric adenocarcinoma harboring KIT Q556_K558del (PMID: 39298692). | 39298692 |
KIT W557_K558del KIT T670I | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT W557_K558del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT T670I (PMID: 18294292). | 18294292 |
KIT L576P | melanoma | unknown | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in initial tumor reduction, but was followed by disease progression at all tumor sites in a patient with metastasized labial melanoma harboring KIT L576P (PMID: 20372153). | 20372153 |
KIT N822I | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822I demonstrated resistance to Gleevec (imatinib) in culture (PMID: 21689725). | 21689725 |
KIT act mut | skin melanoma | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines as second-line therapy for metastatic or unresectable cutaneous melanoma patients with KIT activating mutations (NCCN.org). | detail... |
KIT K642E | vulvar melanoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in partial response in a patient with recurrent vulval melanoma harboring KIT K642E, with reduction of tumor mass by 35% at 12 weeks (PMID: 20372153). | 20372153 |
ABL1 rearrange | myeloid neoplasm | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines for patients with a myeloid/lymphoid neoplasm with eosinophilia harboring a ABL1 rearrangement (NCCN.org). | detail... |
KIT A502_Y503dup KIT D816H | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT D816H demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT V560del KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT V560del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT N822K (PMID: 18294292). | 18294292 |
KIT E554_Y570del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT E554_Y570del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT V654A (PMID: 18294292). | 18294292 |
ABL1 R332W | lung adenocarcinoma | sensitive | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gleevec (imatinib) inhibited growth of a lung adenocarcinoma cell line harboring ABL1 R332W (also reported as R351W) in culture, and inhibited tumor growth in xenograft models (PMID: 26758680). | 26758680 |
KIT D419del | Advanced Solid Tumor | predicted - sensitive | Imatinib | Preclinical - Biochemical | Actionable | In a preclinical study, Gleevec (imatinib) treatment inhibited Kit autophosphorylation in transformed cells expressing KIT D419del in culture (PMID: 16143141). | 16143141 |
KIT K509I | systemic mastocytosis | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in symptom and enzymatic improvements in 2 patients with aggressive systemic mastocytosis harboring KIT K509I, with 1 patient achieving a major response/complete remission, and inhibited growth of primary bone marrow mononuclear cells derived from both patients in culture (PMID: 25139846). | 25139846 |
KIT V560del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) treatment resulted in inhibition of tumor proliferation in a mouse model of gastrointestinal stromal tumor harboring KIT V558del (corresponding to V560del in human) (PMID: 25572173). | 25572173 |
KIT V560del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a complete response in a patient with gastrointestinal stromal tumor harboring KIT V560del, with a progression-free survival of 33.4 months and an overall survival of 46.8 months (PMID: 18294292). | 18294292 |
KIT P551_E554del | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Gleevec (imatinib) in culture (PMID: 25239608). | 25239608 |
KIT V559D | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V559D were sensitive to Gleevec (imatinib), demonstrating decreased cell proliferation in culture and inhibition of Kit, Erk1/2, and Stat3 phosphorylation (PMID: 24205792). | 24205792 |
KIT V559D | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) decreased KIT signaling, and inhibited growth and induced apoptosis of transformed cells expressing KIT V559D in culture (PMID: 21689725). | 21689725 |
KIT V559D | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of transformed cells expressing KIT V559D in culture (PMID: 35194937). | 35194937 |
KIT Y570_Y578del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumors harboring KIT Y570_Y578del, with a progression-free survival of 19.1 months and an overall survival of 53.2 months (PMID: 18294292). | 18294292 |
ABL1 G321L | lung adenocarcinoma | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) inhibited growth of a lung adenocarcinoma cell line harboring ABL1 G321L (also reported as G340L) in culture (PMID: 26758680). | 26758680 |
KIT D816H | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816H were resistant to Gleevec (imatinib) treatment in culture (PMID: 35194937). | 35194937 |
KIT Y570_L576del KIT D816E PTEN T321fs | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib mesylate) did not inhibit Kit, Erk, or Mtor signaling and resulted in minimal tumor inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT D816E, KIT Y570_L576del, and PTEN T321fs, which was established from a patient who did not respond to Gleevec (imatinib mesylate), Sutent (sunitinib), and Nexavar (sorafenib) (PMID: 29100343). | 29100343 |
KIT W557_E561del KIT N822D | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT W557_E561del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT N822D (PMID: 18294292). | 18294292 |
KIT V560D KIT V654A | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560D and KIT V654A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT T670I | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case report, a patient with a gastrointestinal stromal tumor developed disease progression while being treated with Gleevec (imatinib), demonstrating a KIT T670I mutation in the progressive lesion (PMID: 15236194). | 15236194 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines for gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 11 mutations, as adjuvant therapy for patients with localized disease and as first-line therapy for patients with locally advanced, unresectable, or metastatic disease (PMID: 34560242; ESMO.org). | 34560242 detail... |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Imatinib | Phase III | Actionable | In a Phase III trial, a long-term analysis of gastrointestinal stromal tumor (GIST) patients treated with Gleevec (imatinib) demonstrated patients harboring KIT exon 11 mutations had a median progression-free survival of 39.4 months, and median overall survival was not reached, with 69.1% of patients with KIT exon 11 mutations alive at 5 years (PMID: 26687836; NCT00367861). | 26687836 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines for patients with gastrointestinal stromal tumor (GIST) harboring KIT exon 11 mutations (NCCN.org). | detail... |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Imatinib | Phase III | Actionable | In a Phase III trial, Gleevec (imatinib) treatment resulted in longer overall survival (OS) (66 vs 40 months) in gastrointestinal stromal tumor (GIST) patients harboring KIT exon 11 mutations compared to KIT and PDGFRA wild-type patients, while subtypes of KIT exon 11 mutations (deletion, insertation/duplication, point mutation) did not affect OS outcome (PMID: 28196207; NCT00009906). | 28196207 |
KIT V559_T574del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT V559_T574del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT V654A in one lesion (PMID: 18294292). | 18294292 |
KIT T632I | melanoma | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in worsened condition and continued disease progression and metastasis in a patient with metastatic melanoma harboring KIT T632I (PMID: 31043947). | 31043947 |
KIT W557_K558del KIT Y823D | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, two patients with gastrointestinal stromal tumors harboring KIT W557_K558del progressed following an initial response to Gleevec (imatinib), and were found to have acquired the secondary resistance mutation KIT Y823D in one lesion (PMID: 18294292). | 18294292 |
KIT T670I | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT T670I were resistant to treatment with Gleevec (imatinib) in culture (PMID: 33212994). | 33212994 |
KIT T670I | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT T670I demonstrated resistance to Gleevec (imatinib) in culture (PMID: 35194937). | 35194937 |
KIT Q556_W557del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resutled in a partial response in a patient with gastrointestinal stromal tumor harboring KIT Q556_W557del , with a progression-free survival of 26.8 months and an overall survival of 47 months (PMID: 18294292). | 18294292 |
KIT A502_Y503dup KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT N822K was identified as a secondary mutation in a patient with gastrointestinal stromal tumor harboring a primary KIT A502_Y503dup mutation, who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
KIT C809G | Advanced Solid Tumor | predicted - resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, KIT C809G was resistant to inhibition of phosphorylation by Gleevec (imatinib) in cultured cells (PMID: 16954519). | 16954519 |
JAK2 V617F | myeloid leukemia | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed mouse myeloid cells over expressing JAK2 V617F were resistant to Gleevec (imatinib) in culture (PMID: 21224473). | 21224473 |
KIT D816V | systemic mastocytosis | resistant | Imatinib | FDA contraindicated | Actionable | Gleevec (imatinib) is not indicated for patients with aggressive systemic mastocytosis harboring KIT D816V (FDA.gov). | detail... |
KIT I571_D579dup | Advanced Solid Tumor | predicted - resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT I571_D579dup (KIT D579_H580insIDPTQLPYD) were moderately resistant to Gleevec (imatinib) in culture (PMID: 24205792). | 24205792 |
KIT F522C | systemic mastocytosis | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in symptom and pathologic improvements in a patient with systemic mastocytosis harboring germline KIT F522C and inhibited growth of primary bone marrow cells derived from the patient in culture (PMID: 15070706). | 15070706 |
KIT K642E KIT C809G KIT N822H | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, an acquired KIT C809G mutation was identified in a gastrointestinal stromal tumor (GIST) patient harboring KIT K642E and KIT N822H at the time of progression on Gleevec (imatinib) (PMID: 16954519). | 16954519 |
KIT W557_K558del KIT D820A | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT D820A | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT D820A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT V559_V560del | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V559_V560del were sensitive to Gleevec (imatinib), demonstrating decreased cell proliferation in culture (PMID: 24205792). | 24205792 |
KIT V560_L576del | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, a patient derived GIST cell line harboring KIT V560_L576del demonstrated sensitivity to Gleevec (imatinib) in both culture and PDX models, resulting in phosphorylation inhibition of Akt, Kit, and Erk (PMID: 25239608). | 25239608 |
KIT exon9 | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) had no effect on transformed cells expressing a KIT exon 9 mutation in culture (PMID: 25239608). | 25239608 |
KIT V560D KIT D816H | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560D and KIT D816H demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT D816Y | mast cell neoplasm | predicted - resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) were resistant to Gleevec (imatinib) in culture (PMID: 31085175). | 31085175 |
KIT K509I | mastocytosis | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in symptom improvements, liver size reduction, and decrease of enzymatic markers in a patient with familial mastocytosis harboring a germline KIT K509I mutation and inhibited growth of white blood cells derived from the patient in culture (PMID: 16183119). | 16183119 |
KIT P551I KIT M552_V559del KIT Y823D | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT M552_V559del and KIT P551I progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT Y823D (PMID: 18294292). | 18294292 |
KIT Y553S KIT W557_Q575del KIT D820Y | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT D820Y was identified as a secondary mutation in a patient with gastrointestinal stromal tumor harboring primary KIT W557_Q575del (reported as Q556_T574del) and KIT Y553S mutations, who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
KIT V560G | mast cell neoplasm | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of mast cells harboring KIT V560G in culture (PMID: 31085175). | 31085175 |
KIT D579del | thymic carcinoma | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with thymic carcinoma harboring KIT D579del achieved disease stabilization following treatment with Gleevec (imatinib) (PMID: 24419427). | 24419427 |
KIT K558delinsNP | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT H697Y | Advanced Solid Tumor | decreased response | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cell lines overexpressing KIT H697Y demonstrated reduced sensitivity to Gleevec (imatinib mesylate)-induced growth inhibition in culture (PMID: 19861435). | 19861435 |
KIT W557_K558del KIT N822K | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT N822K demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT N822K | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT D816F | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816F were resistant to Gleevec (imatinib mesylate) in culture (PMID: 16397263). | 16397263 |
CTNNB1 act mut | desmoid tumor | sensitive | Imatinib | Clinical Study - Cohort | Actionable | In a retrospective analysis, patients with desmoid fibromatosis harboring CTNNB1 activating exon 3 mutations demonstrated a greater progression arrest rate at 6 months compared to patients with CTNNB1 wild-type tumor when treated with Gleevec (imatinib) (PMID: 26861905). | 26861905 |
KIT W557_K558del KIT D816H | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT W557_K558del progressed after experiencing stable disease on treatment with Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT D816H (PMID: 18294292). | 18294292 |
KIT M541L | chronic leukemia | sensitive | Imatinib | Phase I | Actionable | In Phase I trials, KIT M541L has been associated with response to Gleevec (imatinib) in chronic eosinophilic leukemia, NOS (PMID: 25015329) and mastocytosis (PMID: 18795925). | 25015329 18795925 |
KIT W557_K558delinsCE KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT N822K was identified as a secondary mutation in a patient with gastrointestinal stromal tumor harboring a primary KIT W557_K558delinsCE mutation, who developed resistance to Gleevec (imatinib mesylate) (PMID: 18488160). | 18488160 |
KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, KIT N822K was identified in the tumor of a gastrointestinal stromal tumor patient who was resistant to Gleevec (imatinib) treatment (PMID: 26316776). | 26316776 |
KIT W557_K558del KIT D816E KIT D820V | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT D816E and D820V were identified as secondary mutations in a patient with gastrointestinal stromal tumor harboring KIT W557_K558del who developed resistance to Gleevec (imatinib) (PMID: 18294292). | 18294292 |
KIT V560D | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT D820N | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT D820N was identified as a secondary mutation in the metastatic lesions from a gastrointestinal stromal tumor patient whose disease progressed on Gleevec (imatinib) (PMID: 18628470). | 18628470 |
KIT V560_Y578del KIT V654A | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gleevec (imatinib) failed to decrease cell viability and KIT signaling in a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del and KIT V654A in culture, and did suppress tumor growth in cell line xenograft models (PMID: 32350132). | 32350132 |
KIT P551_K558del | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT V560_Y578del | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, a patient derived GIST cell line harboring KIT V560_Y578del demonstrated sensitivity to Gleevec (imatinib) in culture (PMID: 25239608). | 25239608 |
KIT V560_Y578del | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited cell growth and KIT signaling in a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del in culture, but was less potent compared to AZD3229 (PMID: 32350132). | 32350132 |
KIT exon 11 del KIT D816E | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT D816E in culture (PMID: 31085175). | 31085175 |
KIT W557C KIT Y578C | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib mesylate) inhibited Kit phosphorylation efficiently in transformed human cells over expressing both KIT W557C and KIT Y578C in culture (PMID: 23567324). | 23567324 |
KIT D816V | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816V were resistant to Gleevec (imatinib) treatment in culture (PMID: 35194937). | 35194937 |
KIT D816V | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT D816V demonstrated resistance to Gleevec (imatinib mesylate) in culture (PMID: 15790786). | 15790786 |
KIT D816V | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) treatment did not inhibit proliferation of transformed cells expressing KIT D816V in culture (PMID: 30523507). | 30523507 |
KIT W557Lfs*5 KIT P577del KIT D820G | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, a gastrointestinal stromal tumor patient-derived xenograft (PDX) model harboring KIT P577del, KIT W557Lfs*5, and KIT D820G demonstrated resistance to treatment with Gleevec (imatinib) (PMID: 27777285). | 27777285 |
KIT N655K | Advanced Solid Tumor | predicted - sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N655K demonstrated some sensitivity to Gleevec (imatinib) treatment in culture, resulting in reduced cell viability at high treatment dosages (PMID: 33212994). | 33212994 |
KIT W557_K558del KIT T670I | Advanced Solid Tumor | no benefit | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated no response to treatment with Gleevec (imatinib) in both culture and xenograft models (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT D816H | Advanced Solid Tumor | decreased response | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Gleevec (imatinib) in both culture and xenograft models, resulting in only a slight decrease in tumor volume (PMID: 25239608). | 25239608 |
KIT V555_L576del KIT D820G KIT D820Y | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT D820G and KIT D820Y were identified as secondary mutations in a patient with gastrointestinal stromal tumor harboring a primary KIT V555_L576del mutation, who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
KIT A829P | melanoma | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, melanoma cells expressing KIT A829P demonstrated resistance to treatment with Gleevec (imatinib mesylate) (PMID: 23582185, PMID: 25594040). | 23582185 25594040 |
KIT exon 11 del KIT T670I | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT T670I were resistant to Gleevec (imatinib) in culture (PMID: 31085175). | 31085175 |
KIT N822K | acute myeloid leukemia | decreased response | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring KIT N822K demonstrated reduced response to growth inhibition by Gleevec (imatinib) compared to GIST cells harboring KIT exon 11 deletion in culture (PMID: 31085175). | 31085175 |
KIT D419del | mastocytosis | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resolved symptoms and stopped disease progression after 32 months in a pediatric patient with progressive cutaneous mastocytosis harboring a somatic KIT D419del and a germline S840N mutation (PMID: 18567837). | 18567837 |
KIT C443S | mucosal melanoma | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with mucosal melanoma harboring KIT C443S demonstrated a substantial response to Gleevec (imatinib) in the first two weeks and then developed progression at 15 weeks (PMID: 25003536). | 25003536 |
KIT V560D KIT D820A | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560D and KIT D820A demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, three patients with gastrointestinal stromal tumors harboring KIT W557_K558del progressed following an initial response to Gleevec (imatinib), and were found to have acquired the secondary resistance mutation KIT V654A (PMID: 18294292). | 18294292 |
KIT P551I KIT M552_V559del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumors harboring KIT M552_V559del and KIT P551I, with a progression-free survival of 9 months and an overall survival of 19.5 months (PMID: 18294292). | 18294292 |
KIT W557_K558del KIT D820G | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT exon 11 del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Phase III | Actionable | In a Phase III trial, gastrointestinal stromal tumor patients harboring KIT exon 11 deletions or indels demonstrated improved recurrence-free survival (RFS) with 3-year adjuvant Gleevec (imatinib) treatment (5-year RFS, 70%), compared to patients receiving 1-year treatment (5-year RFS, 41.3%) (PMID: 28334365). | 28334365 |
KIT exon 11 del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited Kit phosphorylation and proliferation of gastrointestinal stromal tumor cells harboring KIT exon 11 deletion in culture (PMID: 31085175). | 31085175 |
KIT exon 11 del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Phase III | Actionable | In a Phase III trial, 3-year adjuvant Gleevec (imatinib) treatment resulted in an improved 10-year overall survival rate (86% vs 64%, HR=0.34, p=0.0007) and 10-year recurrence-free survival rate (47% vs 29%, HR=0.48, p<0.001) compared to 1-year adjuvant treatment in patients with gastrointestinal stromal tumors harboring KIT exon 11 deletion or indel mutations (PMID: 37014660; NCT00116935). | 37014660 |
KIT T670E | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT T670E demonstrated resistance to Gleevec (imatinib) in culture (PMID: 35194937). | 35194937 |
KIT exon9 | gastrointestinal stromal tumor | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines for patients with gastrointestinal stromal tumor (GIST) harboring KIT exon 9 mutations (NCCN.org). | detail... |
KIT exon9 | gastrointestinal stromal tumor | sensitive | Imatinib | Guideline | Actionable | Gleevec (imatinib) is included in guidelines for gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 9 mutations, as adjuvant therapy for patients with localized disease and as first-line therapy for patients with locally advanced, unresectable, or metastatic disease (PMID: 34560242; ESMO.org). | 34560242 detail... |
KIT M552_D572del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, two patients with gastrointestinal stromal tumors harboring KIT M552_D572del progressed following an initial response to Gleevec (imatinib), and were found to have acquired the secondary resistance mutation KIT V654A (PMID: 18294292). | 18294292 |
KIT W557_E561del | gastrointestinal stromal tumor | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to partial responses in two patients with gastrointestinal stromal tumors harboring KIT W557_E561del, with a progression-free survival (PFS) of 10.7 mo and overall survival (OS) of 14.9 mo in one patient, and a PFS of 32.2 mo and OS of 34.4 mo in the second patient (PMID: 18294292). | 18294292 |
KIT W557_E561del | gastrointestinal stromal tumor | sensitive | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib) inhibited tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_E561del with overexpression of GPR20 (IHC score 3+) (PMID: 33579785). | 33579785 |
KIT V555_D572del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumor harboring KIT V555_D572del, with a progression-free survival of 49.4 mo and an overall survival of 59.3 mo (PMID: 18294292). | 18294292 |
KIT W557_K558del | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Gleevec (imatinib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT K509I | gastrointestinal stromal tumor | no benefit | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in stable disease at 9 months in a patient with advanced gastrointestinal stromal tumor harboring a germline KIT K509I mutation, which was later discontinued due to adverse effects and lack of response (PMID: 23610110). | 23610110 |
KIT V559_T574del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumors harboring KIT V559_T574del, with a progression-free survival of 28 months and an overall survival of 54.9 months (PMID: 18294292). | 18294292 |
KIT N822K | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N822K were resistant to treatment with Gleevec (imatinib) in culture (PMID: 24205792). | 24205792 |
KIT over exp | seminoma | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) in conjunction with third-line chemotherapy resulted in a complete response in a patient with stage IV chemoresistant pure seminoma with KIT overexpression (PMID: 18751412). | 18751412 |
KIT K558N KIT V560del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumors harboring KIT K558N and KIT V560del (reported as KIT V559del), with a progression-free survival of 23.4 months and an overall survival of 54.7 months (PMID: 18294292). | 18294292 |
KIT W557_K558del KIT V654A | Advanced Solid Tumor | no benefit | Imatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated no response to treatment with Gleevec (imatinib) in both culture and xenograft models (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT Y823D | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT Y823D demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT W557G | extraskeletal myxoid chondrosarcoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in stable disease lasting at least 3 years in a patient with extraskeletal myxoid chondrosarcoma harboring KIT W557G (PMID: 34446510). | 34446510 |
KIT V559G | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of transformed cells expressing KIT V559G in culture (PMID: 35194937). | 35194937 |
KIT W557_K558del KIT A829P | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT A829P demonstrated resistance to Gleevec (imatinib) in culture (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT A829P | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT D816E | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of transformed cells expressing KIT D816E in culture (PMID: 35194937). | 35194937 |
KIT D820Y | melanoma | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib mesylate) failed to inhibit MNK pathway activation and proliferation of melanoma cell lines harboring KIT D820Y in culture (PMID: 29035277). | 29035277 |
KIT V560_D572del | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment led to a partial response in a patient with gastrointestinal stromal tumors harboring KIT V560_D572del, with a progression-free survival of 16.5 months and an overall survival of 57.4 months (PMID: 18294292). | 18294292 |
KIT V559D KIT Y823D | Advanced Solid Tumor | no benefit | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) treatment in a mouse model with cells expressing KIT V559D and KIT Y823D resulted in shortened survival (PMID: 24205792). | 24205792 |
KIT Y578C | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib mesylate) inhibited Kit phosphorylation efficiently in transformed human cells over expressing KIT Y578C in culture (PMID: 23567324). | 23567324 |
KIT L576P | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib) inhibited proliferation of transformed cells expressing KIT L576P in culture (PMID: 35194937). | 35194937 |
KIT V559A | melanoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment in a patient with metastatic melanoma resulted in regression of the lung metastasis, which harbored KIT V559A; however, neither the primary tumor or lymph node metastasis responded, which had wild-type KIT (PMID: 19812602). | 19812602 |
KIT T417_D419delinsI | Advanced Solid Tumor | conflicting | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT T417_D419delinsI were resistant to treatment with Gleevec (imatinib) in culture (PMID: 24205792). | 24205792 |
KIT T417_D419delinsI | Advanced Solid Tumor | conflicting | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gleevec (imatinib mesylate) inhibited Kit phosphorylation in transformed cells over expressing KIT T417_D419delinsI in culture (PMID: 16015387). | 16015387 |
KIT positive | prostate neuroendocrine neoplasm | no benefit | Imatinib | Preclinical | Actionable | In a preclinical study, a prostate neuroendocrine tumor mouse model expressing Kit did not respond to Gleevec (imatinib), a result of impaired signaling of the Kit pathway (PMID: 27980106). | 27980106 |
KIT A502_Y503dup | Advanced Solid Tumor | sensitive | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT A502_Y503dup (Y503_F504insAY) were sensitive to Gleevec (imatinib) in culture, demonstrating decreased cell proliferation (PMID: 24205792). | 24205792 |
CTNNB1 T41A | desmoid tumor | sensitive | Imatinib | Clinical Study - Cohort | Actionable | In a retrospective analysis, patients with desmoid fibromatosis harboring CTNNB1 T41A demonstrated a greater progression arrest rate at 6 months (70%) compared to patients with CTNNB1 wild-type (45%) when treated with Gleevec (imatinib) (PMID: 26861905). | 26861905 |
KIT Y553N | thymic carcinoma | sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic thymic carcinoma harboring KIT Y553N demonstrated improved clinical performance and reduction in metastatic lesions following treatment with Gleevec (imatinib) (PMID: 21969494). | 21969494 |
KIT V555_D572del KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT V555_D572del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT N822K (PMID: 18294292). | 18294292 |
KIT A502_Y503dup KIT D820E | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib mesylate) did not inhibit Kit, Erk, or Mtor signaling and resulted in minimal (7.4%) tumor inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup and KIT D820E, which was established from a patient who did not respond to Gleevec (imatinib mesylate) and Sutent (sunitinib) (PMID: 29100343). | 29100343 |
KIT K558_V560del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT V654A was identified as a secondary mutation in a patient with gastrointestinal stromal tumor harboring a primary KIT K558_V560del mutation, who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
KIT positive | germ cell cancer | no benefit | Imatinib | Phase II | Actionable | In a small Phase II study, 6 patients with KIT-positive refractory germ cell tumors treated with Gleevec (imatinib) experienced no significant antitumor activity (PMID: 16462496). | 16462496 |
KIT N505I | melanoma | predicted - sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) decreased phosphorylation of KIT, AKT, and ERK in melanocytes expressing KIT N505I in culture (PMID: 24317392). | 24317392 |
KIT T670I | melanoma | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, melanoma cells expressing KIT T670I demonstrated resistance to treatment with Gleevec (imatinib mesylate) (PMID: 23582185, PMID: 25594040). | 23582185 25594040 |
KIT N655K | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor (GIST) harboring a germline KIT N655K mutation, associated with hereditary GIST syndrome, demonstrated slow disease progression for 12 months while on treatment with Gleevec (imatinib) at 400mg/d, and upon disease progression following surgery and 15 months of Sutent (sunitinib) treatment, was rechallenged with Gleevec (imatinib) at 800mg/d and remained stable for a further 9 months (PMID: 33212994). | 33212994 |
KIT V560del KIT over exp | thymic carcinoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case report, a patient with metastatic thymic carcinoma harboring KIT V560del with KIT over expression initially demonstrated stable disease and reduction in metastatic lesions following treatment with Gleevec (imatinib), but progressed after 6 months (PMID: 15201427). | 15201427 |
KIT V559D KIT T670I | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V559D and T670I were resistant to Gleevec (imatinib) treatment in culture (PMID: 35194937). | 35194937 |
KIT D816V | hematologic cancer | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, a mouse myeloid cell line expressing KIT D816V demonstrated resistance to Gleevec (imatinib) in culture (PMID: 12481435). | 12481435 |
CSF3R T618I | hematologic cancer | no benefit | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed bone marrow cells expressing CSF3R T618I were not sensitive to Gleevec (imatinib) in culture, demonstrating similar colony formation compared to treatment controls (PMID: 29572350). | 29572350 |
KIT V560_L576del KIT V654A | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT V560_L576del and V654A with overexpression of GPR20 (IHC score 3+) demonstrated resistance to treatment with Gleevec (imatinib) (PMID: 33579785). | 33579785 |
KIT W557_E561del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, two patients with gastrointestinal stromal tumors harboring KIT W557_E561del progressed following an initial response to Gleevec (imatinib), and were found to have acquired the secondary resistance mutation KIT V654A (PMID: 18294292). | 18294292 |
KIT D816Y | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816Y were resistant to Gleevec (imatinib mesylate) in culture (PMID: 16397263). | 16397263 |
KIT D816Y | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816Y were resistant to treatment with Gleevec (imatinib) in culture (PMID: 24205792). | 24205792 |
KIT exon11 KIT T670I | gastrointestinal stromal tumor | resistant | Imatinib | Preclinical - Pdx | Actionable | In a preclinical study, Gleevec (imatinib mesylate) did not inhibit Kit, Erk signaling and resulted in limited (53.9%) tumor inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT exon 11 mutation (K550_splice) and KIT T670I, which was established from a patient who did not respond to Gleevec (imatinib mesylate) (PMID: 29100343). | 29100343 |
KIT exon11 | melanoma | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, Gleevec (imatinib) treatment resulted in a partial response in a patient with metastastic anal melanoma harboring a 21 base-pair duplication in KIT exon 11, and reduced pulmonary metastasis by 60% (PMID: 20372153). | 20372153 |
KIT V560del | Advanced Solid Tumor | sensitive | Imatinib | Preclinical | Actionable | In a preclinical study, Gleevec (imatinib) inhibited growth of transformed cell lines over expressing KIT V560del in culture (PMID: 19861435). | 19861435 |
KIT V555_D572del KIT N822Y | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with gastrointestinal stromal tumor harboring KIT V555_D572del progressed following an initial response to Gleevec (imatinib), and was found to have acquired the secondary resistance mutation KIT N822Y (PMID: 18294292). | 18294292 |
KIT V560E | gastrointestinal stromal tumor | predicted - sensitive | Imatinib | Case Reports/Case Series | Actionable | In a clinical case study, neoadjuvant Gleevec (imatinib) treatment resulted in decreased tumor size with a maximal response at 12 months in a patient with gastrointestinal stromal tumor (GIST) harboring KIT V560E, allowing for surgical resection (PMID: 34250403). | 34250403 |
KIT W557_K558del KIT D816G | Advanced Solid Tumor | resistant | Imatinib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Gleevec (imatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT V559A | gastrointestinal stromal tumor | predicted - resistant | Imatinib | Case Reports/Case Series | Actionable | In a clinical study, KIT V559A was identified as a secondary mutation in a patient with gastrointestinal stromal tumor who developed resistance to Gleevec (imatinib) (PMID: 18488160). | 18488160 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT00471497 | Phase III | Nilotinib Imatinib | A Study of Imatinib Versus Nilotinib in Adult Patients With Newly Diagnosed Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP) (ENESTnd) | Completed | USA | TUR | SWE | SVK | POL | NOR | NLD | ITA | HUN | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CHE | CAN | BRA | BEL | AUT | ARG | 13 |
NCT02709083 | Phase II | Dasatinib Nilotinib Imatinib | Dasatinib or Nilotinib Followed by Imatinib in Patients With Newly Diagnosed, Chronic Phase Chronic Myeloid Leukemia | Terminated | USA | 0 |
NCT04307576 | Phase III | Imatinib Blinatumomab Inotuzumab ozogamicin | A Treatment Study Protocol for Participants 0-45 Years With Acute Lymphoblastic Leukaemia | Recruiting | SWE | NOR | NLD | LTU | ISL | IRL | GBR | FRA | FIN | EST | DNK | DEU | BEL | 1 |
NCT01593254 | Phase II | Imatinib Dasatinib | Study of Dasatinib vs Imatinib in Patients With Chronic Myeloid Leukemia (CML) Who Did Not Have Favorable Response to Imatinib (DASCERN) | Completed | USA | POL | ITA | HUN | FRA | ESP | CZE | CAN | BRA | BEL | AUT | ARG | 3 |
NCT05493215 | Phase II | Imatinib | Imatinib TDM in GIST | Recruiting | USA | 0 |
NCT03688568 | Phase II | Imatinib | Study of Imatinib in Children With Neurofibromatosis and Airway Tumors | Withdrawn | USA | 0 |
NCT05152472 | Phase II | Imatinib Atezolizumab + Imatinib | A Prospective, Randomized, Multicenter, Comparative Study of the Efficacy of Imatinib Resumption Combined With Atezolizumab Versus Imatinib Resumption Alone in Patients With Unresectable Advanced Gastrointestinal Stromal Tumors (GIST) After Failure of Standard Treatments (ATEZOGIST) | Recruiting | FRA | 0 |
NCT05413915 | Phase III | Asciminib + Imatinib Imatinib | Asciminib Used in Consolidation With Imatinib vs. Imatinib to Achieve TFR in CP-CML | Recruiting | CAN | 0 |
NCT06061094 | Phase II | Blinatumomab + Ponatinib Imatinib Blinatumomab + Imatinib Ponatinib | Randomized Trial in Adult de Novo Ph Positive ALL With Chemotherapy, Imatinib or Ponatinib, Blinatumomab and SCT (GMALL-EVOLVE) | Recruiting | DEU | 0 |
NCT01316250 | Phase II | Imatinib Nilotinib | Gleevec as Maintenance Therapy After Cytogenetic Response With Nilotinib in Newly Diagnosed Chronic Myelogenous Leukemia | Recruiting | LBN | 0 |
NCT02602314 | FDA approved | Imatinib Nilotinib | Sustained Treatment-free Remission in BCR-ABL+ Chronic Myeloid Leukemia (SUSTRENIM) | Unknown status | NLD | ITA | 0 |
NCT03578367 | Phase II | Imatinib Nilotinib Asciminib + Imatinib | Study of Efficacy and Safety of Asciminib in Combination With Imatinib in Patients With Chronic Myeloid Leukemia in Chronic Phase (CML-CP) | Active, not recruiting | USA | POL | ITA | GBR | FRA | ESP | DNK | DEU | CZE | CAN | AUT | 4 |
NCT02326311 | Phase III | Dasatinib Nilotinib Imatinib | Optimization of TKIs Treatment and Quality of Life in Ph+ CML Patients >=60 Years in Deep Molecular Response | Completed | ITA | 0 |
NCT01319981 | Phase II | Pegfilgrastim Imatinib Filgrastim Rituximab Doxorubicin Dexamethasone Vincristine Sulfate Cyclophosphamide | Hyper-CVAD With Liposomal Vincristine in Acute Lymphoblastic Leukemia | Completed | USA | 0 |
NCT05245968 | Phase I | Imatinib Sunitinib Pimitespib Imatinib + Pimitespib | A Study of Pimitespib in Combination With Imatinib in Patients With GIST (CHAPTER-GIST-101) | Recruiting | AUS | 4 |
NCT02551718 | Phase I | Bosutinib Irinotecan Romidepsin Busulfan Melphalan Nilotinib Crizotinib Cytarabine Mitoxantrone Dasatinib Pazopanib Paclitaxel Clofarabine Hydroxyurea Tretinoin Carfilzomib Nelarabine Bexarotene Pentostatin Everolimus Cabozantinib Mercaptopurine Methotrexate Cladribine Thioguanine Daunorubicin Ponatinib Etoposide Afatinib Gefitinib Gemcitabine Regorafenib Arsenic trioxide Trametinib Imatinib Erlotinib Dabrafenib Decitabine Axitinib Azacitidine Ruxolitinib Fludarabine Lapatinib Ceritinib Sirolimus Sorafenib Lomustine Sunitinib Cabazitaxel Temsirolimus Topotecan Bortezomib Pralatrexate | High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia | Completed | USA | 0 |
NCT03023046 | Phase II | Rituximab Doxorubicin Etoposide Imatinib Dasatinib Cyclophosphamide Prednisone Vincristine Sulfate | Etoposide, Prednisone, Vincristine Sulfate, Cyclophosphamide, and Doxorubicin in Treating Patients With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma | Completed | USA | 0 |
NCT03469011 | Phase I | Imatinib | A Study to Try to Bring Back Radioiodine Sensitivity in Patients With Advanced Thyroid Cancer. | Recruiting | CAN | 0 |
NCT02538926 | Phase II | Imatinib Rituximab Cyclophosphamide Prednisone Doxorubicin + Etoposide + Vincristine Sulfate Asparaginase | Etoposide, Prednisone, Vincristine Sulfate, Cyclophosphamide, and Doxorubicin Hydrochloride With Asparaginase in Treating Patients With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma | Withdrawn | USA | 0 |
NCT03007147 | Phase III | Pegaspargase Methotrexate Leucovorin Cytarabine Mercaptopurine Thioguanine Vincristine Sulfate Cyclophosphamide Imatinib Ifosfamide Dexrazoxane Daunorubicin Dexamethasone Methylprednisolone Etoposide Prednisolone Doxorubicin | Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia | Active, not recruiting | USA | SWE | NZL | NLD | ITA | ISR | FRA | FIN | DEU | CZE | CHE | CAN | BEL | AUT | AUS | 4 |
NCT02788201 | Phase II | Erlotinib Thiotepa Imatinib Dacarbazine Arsenic trioxide Idarubicin Mitomycin C Thioguanine Mercaptopurine Methotrexate Cladribine Epirubicin Gemcitabine Doxorubicin Bleomycin Etoposide Gefitinib Daunorubicin Lomustine Sorafenib Sunitinib Ifosfamide Asparaginase Ixabepilone Abiraterone Azacitidine Ruxolitinib Decitabine Axitinib Estramustine Floxuridine Lapatinib Carmustine Fludarabine Nilotinib Cisplatin Vismodegib Vandetanib Melphalan Busulfan Carboplatin Toremifene Crizotinib Dactinomycin Temsirolimus Vorinostat Romidepsin Fluorouracil Irinotecan Bortezomib Tamoxifen Topotecan Chlorambucil Pentostatin Eribulin Carfilzomib Vemurafenib Hydroxyurea Exemestane Vincristine Sulfate Dasatinib Mitoxantrone Vinblastine Cytarabine Tretinoin Clofarabine Teniposide Docetaxel Pazopanib Oxaliplatin Streptozocin Paclitaxel Bendamustine Mechlorethamine Mitotane | Genomic Based Assignment of Therapy in Advanced Urothelial Carcinoma | Completed | USA | 0 |
NCT00812240 | Phase III | Masitinib Imatinib | A Phase 3 Study to Evaluate Efficacy and Safety of Masitinib in Comparison to Imatinib in Patients With Gastro-Intestinal Stromal Tumour in First Line Medical Treatment | Terminated | USA | LBN | FRA | 0 |
NCT03193281 | Phase II | Imatinib Dasatinib | KISS Study: Kinase Inhibition With Sprycel Start up (KISS) | Active, not recruiting | NZL | 0 |
NCT05009927 | Phase II | Imatinib | Efficiency of Imatinib Treatment After 10 Years of Treatment in Patients With Gastrointestinal Stromal Tumours (GIST) (Gist-Ten) | Recruiting | FRA | 0 |
NCT00290485 | Phase II | Imatinib | Gleevec Administered Preoperatively to Reduce Gastrointestinal Stromal Tumor (GIST) | Unknown status | CAN | 0 |
NCT04971226 | Phase III | Asciminib Bosutinib Imatinib Dasatinib Nilotinib | A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP | Active, not recruiting | USA | SWE | SVK | NOR | NLD | ITA | ISR | HUN | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CHE | CAN | BGR | BEL | AUT | AUS | 8 |
NCT04722848 | Phase III | Blinatumomab + Ponatinib Imatinib | Sequential Treatment With Ponatinib and Blinatumomab vs Chemotherapy and Imatinib in Newly Diagnosed Adult Ph+ ALL | Recruiting | ITA | 0 |
NCT02130557 | Phase III | Bosutinib Imatinib | A Multicenter Phase 3, Open-Label Study of Bosutinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia | Completed | USA | SWE | SVK | POL | NOR | NLD | ITA | ISR | HUN | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CAN | BEL | AUS | 7 |
NCT01244750 | Phase I | Imatinib Dasatinib Nilotinib | Studying First Line Treatment of Chronic Myeloid Leukemia (CML) in a Real-world Setting | Completed | USA | NLD | ITA | FRA | ESP | DEU | 2 |
NCT04817956 | Phase II | Ceritinib Melphalan Cobimetinib + Vemurafenib Alectinib Pemigatinib Entrectinib Bortezomib Dostarlimab-gxly Atezolizumab Alpelisib Atezolizumab + Bevacizumab Olaparib Selpercatinib Capmatinib Dactinomycin Dabrafenib + Trametinib Vismodegib Niraparib Imatinib Pertuzumab/trastuzumab/hyaluronidase-zzxf | Improving Public Cancer Care by Implementing Precision Medicine in Norway (IMPRESS-N) | Recruiting | NOR | 0 |
NCT02611492 | Phase III | Mercaptopurine + Methotrexate + Nilotinib Cytarabine + Dexamethasone + Filgrastim + Methotrexate + Nilotinib + Vincristine Sulfate Imatinib | A Phase III Randomized Trial of the Reduction of Chemotherapy in Philadelphia Chromosome-positive ALL of Young Adults (GRAAPH2014) | Recruiting | FRA | 0 |
NCT02260505 | Phase III | Imatinib | Efficiency of Imatinib Treatment Maintenance or Interruption After 3 Years of Adjuvant Treatment in Patients With Gastrointestinal Stromal Tumours (GIST) (ImadGist) | Completed | FRA | 0 |
NCT02177825 | Phase II | Imatinib | Study of Imatinib Mesylate in Neurofibromatosis Type I Patients Aged 2 to 21 With Plexiform Neurofibromas | Terminated | CAN | 0 |
NCT03878524 | Phase I | Oxaliplatin Palbociclib Vemurafenib Sirolimus Tretinoin Celecoxib Ipilimumab Ruxolitinib Dasatinib Abiraterone Idelalisib Trametinib Imatinib Erlotinib Carboplatin Olaparib Panobinostat Bortezomib Afatinib Fluorouracil Vorinostat Pembrolizumab Leucovorin Enzalutamide Ponatinib Nivolumab Everolimus Sunitinib Cabazitaxel Cabozantinib Lenvatinib Pertuzumab Sorafenib Venetoclax Bevacizumab | A Personalized Medicine Study for Patients With Advanced Cancer of the Breast, Prostate, Pancreas or Those With Refractory Acute Myelogenous Leukemia (SMMART) | Terminated | USA | 0 |
NCT02352558 | Phase I | Imatinib Napabucasin Bortezomib Ibrutinib Dexamethasone | A Study of BBI608 in Adult Patients With Advanced, Refractory Hematologic Malignancies | Completed | USA | 0 |