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Therapy Name Regorafenib
Synonyms
Therapy Description

Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Regorafenib Stivarga BAY 73-4506 BRAF Inhibitor 25 CRAF Inhibitor 12 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 RET Inhibitor 53 VEGFR Inhibitor (Pan) 36 VEGFR2 Inhibitor 37 Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KIT exon17 melanoma sensitive Regorafenib Case Reports/Case Series Actionable In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). 37741071
VHL del renal cell carcinoma predicted - sensitive Regorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Stivarga (regorafenib) inhibited angiogenesis and tumor growth in cell line xenograft models of renal cell carcinoma harboring VHL gene deletion (PMID: 21170960). 21170960
KIT exon 11 del KIT D816E gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT D816E in culture (PMID: 31085175). 31085175
KIT D816Y mast cell neoplasm predicted - resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). 31085175
KIT K558delinsNP Advanced Solid Tumor sensitive Regorafenib Preclinical Actionable In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608). 25239608
KIT V560G KIT D816V mast cell neoplasm resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, mast cells harboring both KIT D816V and KIT V560G were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). 31085175
KIT P551_E554del Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). 25239608
KIT V560_L576del KIT V654A gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) inhibited tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT V560_L576del and V654A with overexpression of GPR20 (IHC score 3+) (PMID: 33579785). 33579785
KIT W557_K558del KIT T670I Advanced Solid Tumor decreased response Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Stivarga (regorafenib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 25239608). 25239608
KIT W557_K558del KIT T670I Advanced Solid Tumor decreased response Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Stivarga (regorafenib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). 32350132
MAP2K1 I111S Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 I111S displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT W557_K558del KIT D820A Advanced Solid Tumor conflicting Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT D820A were sensitive to treatment with Stivarga (regorafenib), demonstrating reduced cell viability in culture (PMID: 32350132). 32350132
KIT W557_K558del KIT D820A Advanced Solid Tumor conflicting Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). 25239608
BRAF V600E PIK3CA P449T colorectal cancer resistant Regorafenib Preclinical Actionable In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). 25838391
BRAF V600E colorectal cancer sensitive Regorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture and suppressed angiogenesis and tumor growth in cell line xenograft models (PMID: 21170960). 21170960
KIT V560_Y578del gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited growth of a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del in culture, but was less potent compared to AZD3229 (PMID: 32350132). 32350132
KIT exon9 melanoma predicted - sensitive Regorafenib Case Reports/Case Series Actionable In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). 37741071
KIT W557_K558del KIT Y823D gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) inhibited tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and KIT Y823D (PMID: 32350132). 32350132
KIT V560G mast cell neoplasm sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of mast cells harboring KIT V560G in culture (PMID: 31085175). 31085175
KIT K642E KIT N822K gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) suppressed tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT K642E and KIT N822K, but was less potent in comparison to treatment with AZD3229 (PMID: 32350132). 32350132
BRAF mutant colorectal cancer no benefit Regorafenib Phase II Actionable In a Phase II clinical trial (PREVIUM), Stivarga (regorafenib) treatment resulted in 0% (0/15) 6-month progression free survival (PFS), a 2.2-month median PFS, and a median overall survival of 3.3 months in metastatic colorectal cancer patients with KRAS (n=9), NRAS (n=3) or BRAF (n=2) mutations who failed first line therapy; however, the trial was terminated early due to poor accrual (PMID: 30120161; NCT02175654). 30120161
KIT A502_Y503dup KIT V654A Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT V654A demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). 32350132
MAP2K1 Q56P Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 Q56P displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT T670I Advanced Solid Tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT T670I demonstrated sensitivity to Stivarga (regorafenib) treatment in culture, resulting in reduced cell viability (PMID: 33212994). 33212994
FGFR1 amp FGFR2 amp breast cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). 33563752
KIT exon11 gastrointestinal stromal tumor sensitive Regorafenib Phase II Actionable In a Phase II clinical trial, treatment with Stivarga (regorafenib) resulted in a clinical benefit rate of 76% (25/33), a median progression-free survival (PFS) of 13.2 months, and a median overall survival of 25 months in patients with gastrointestinal stromal tumors, with patients with KIT exon 11 mutations demonstrating the longest PFS of 13.4 months (PMID: 27371698). 27371698
KIT exon11 gastrointestinal stromal tumor sensitive Regorafenib Guideline Actionable Stivarga (regorafenib) is included in guidelines as third-line or subsequent therapy for locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 11 mutations (PMID: 34560242; ESMO.org). 34560242 detail...
KIT exon13 melanoma sensitive Regorafenib Case Reports/Case Series Actionable In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). 37741071
KIT exon9 Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, Stivarga (regorafineb) had no effect on transformed cells expressing a KIT exon 9 mutation in culture (PMID: 25239608). 25239608
KIT N655K Advanced Solid Tumor decreased response Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT N655K demonstrated a reduced response to Stivarga (regorafenib) treatment compared to cells expressing KIT T670I in culture (PMID: 33212994). 33212994
FGFR3 fusion urinary bladder cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, bladder cancer cell lines harboring an FGFR3 fusion were sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth (PMID: 33563752). 33563752
KIT W557_K558del KIT D816G Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). 25239608
KIT exon11 melanoma sensitive Regorafenib Phase II Actionable In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). 37741071
KIT act mut melanoma predicted - sensitive Regorafenib Case Reports/Case Series Actionable In a clinical case study, Stivarga (regorafenib) treatment demonstrated safety and preliminary activity in patients with melanoma harboring activating mutations in KIT, resulting in an overall response rate of 100% (7/7, 1 complete and 6 partial responses), with median duration of response and median progression-free survival not reached and response ongoing in 4 patients at a median follow-up of 43 weeks (Ann Oncol (2024) 35 (suppl_2): S743-S744). detail...
KIT W557_K558del KIT Y823D Advanced Solid Tumor predicted - sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT Y823D demonstrated sensitivity to treatment with Stivarga (regorafenib), but was decreased compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). 32350132
RET C634W thyroid cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of thyroid cancer cells harboring RET C634W in culture (PMID: 21170960). 21170960
KIT V560_Y578del KIT V654A gastrointestinal stromal tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del and KIT V654A demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). 32350132
KIT exon11 KIT T670I gastrointestinal stromal tumor predicted - sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) inhibited Kit signaling, resulted in tumor growth 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 exon 11 del gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited Kit phosphorylation and proliferation of gastrointestinal stromal tumor cells harboring KIT exon 11 deletion in culture (PMID: 31085175). 31085175
FGFR2 amp FGFR2 over exp stomach cancer no benefit Regorafenib Case Reports/Case Series Actionable In a Phase II trial, gastric cancer patients (n=3/35) with FGFR2 amplification and FGFR2 overexpression did not achieve an objective response when treated with Stivarga (regorafenib) (PMID: 33563752). 33563752
KIT D816V Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816V were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). 31085175
KIT W557_K558del KIT N822K Advanced Solid Tumor conflicting Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT N822K was sensitive to treatment with Stivarga (regorafenib), demonstrating decreased cell viability in culture (PMID: 32350132). 32350132
KIT W557_K558del KIT N822K Advanced Solid Tumor conflicting Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). 25239608
MAP2K1 K57N Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 K57N displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT D816H Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, KIT D816H demonstrated resistance to Stivarga (regorafenib) in an in vitro assay, and conferred secondary resistance to Stivarga (regorafenib) in transformed cells expressing other KIT mutations (PMID: 25239608). 25239608
KIT V560D KIT D820A Advanced Solid Tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) treatment resulted in decreased viability of transformed cells expressing KIT V560D and KIT D820A in culture, but was less effective compared to other treatments (PMID: 32350132). 32350132
KIT V560D KIT D816H Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D and KIT D816H demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). 32350132
FGFR1 over exp stomach cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, treatment with Stivarga (regorafenib) in an FGFR1-overexpressing gastric cancer cell line resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). 33563752
MAP2K1 V211D Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 V211D displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT P551_K558del Advanced Solid Tumor sensitive Regorafenib Preclinical Actionable In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608). 25239608
KIT A502_Y503dup KIT D816H Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT D816H demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). 32350132
FGFR2 amp colorectal cancer predicted - sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified colorectal cancer cells in culture (PMID: 29573334). 29573334
FGFR2 amp colorectal cancer predicted - sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). 33563752
KIT W557_K558del KIT A829P Advanced Solid Tumor conflicting Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). 25239608
KIT W557_K558del KIT A829P Advanced Solid Tumor conflicting Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT W557_K558del and KIT A829P were sensitive to treatment with Stivarga (regorafenib), but demonstrated a decreased response compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). 32350132
KIT A502_Y503dup Advanced Solid Tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) treatment resulted in decreased viability of transformed cells expressing KIT A502_Y503dup in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132). 32350132
KIT W557_K558del KIT D816H Advanced Solid Tumor decreased response Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). 25239608
KIT V560D KIT V654A Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT V560D and KIT V654A demonstrated resistance to treatment with Stivarga (regorafenib) in culture (PMID: 32350132). 32350132
KIT Y570_L576del KIT D816E PTEN T321fs gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) inhibited Kit, Erk, and Mtor signaling, resulted in tumor growth 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
NRAS mutant colorectal cancer no benefit Regorafenib Phase II Actionable In a Phase II clinical trial (PREVIUM), Stivarga (regorafenib) treatment resulted in 0% (0/15) 6-month progression free survival (PFS), a 2.2-month median PFS, and a median overall survival of 3.3 months in metastatic colorectal cancer patients with KRAS (n=9), NRAS (n=3) or BRAF (n=2) mutations who failed first line therapy; however, the trial was terminated early due to poor accrual (PMID: 30120161; NCT02175654). 30120161
KIT N822K acute myeloid leukemia sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). 31085175
KIT K642E gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring KIT K642E in culture (PMID: 21170960). 21170960
FGFR2 amp stomach cancer sensitive Regorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified gastric cancer cell lines in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 29573334). 29573334
FGFR2 amp stomach cancer sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, treatment with Stivarga (regorafenib) in gastric cancer cell lines harboring FGFR2 amplification resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). 33563752
FBXW7 R505C colorectal cancer resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, colorectal cell lines with FBXW7 R505C demonstrated acquired resistance in regorafenib (PMID: 27399335). 27399335
KIT V560D Advanced Solid Tumor sensitive Regorafenib Preclinical Actionable In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608). 25239608
KIT W557_K558del KIT V654A Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated resistance to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). 25239608
KIT A502_Y503dup gastrointestinal stromal tumor predicted - sensitive Regorafenib Preclinical - Pdx Actionable In a preclinical study, Stivarga (regorafenib) did not significantly inhibit Kit, Erk, or Mtor signaling, but resulted in tumor growth 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
MAP2K1 F129L Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT exon 11 del KIT T670I gastrointestinal stromal tumor sensitive Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT T670I in culture (PMID: 31085175). 31085175
MAP2K1 F53L Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F53L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT exon9 gastrointestinal stromal tumor sensitive Regorafenib Guideline Actionable Stivarga (regorafenib) is included in guidelines as third-line or subsequent therapy for locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 9 mutations (PMID: 34560242; ESMO.org). 34560242 detail...
KIT W557_K558del KIT D820G Advanced Solid Tumor resistant Regorafenib Preclinical Actionable In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). 25239608
MAP2K1 C121S Advanced Solid Tumor resistant Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 C121S displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KIT W557_K558del Advanced Solid Tumor sensitive Regorafenib Preclinical Actionable In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608). 25239608

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01896856 Phase Ib/II Guadecitabine + Irinotecan Regorafenib Phase I Study of SGI-110 With Irinotecan Followed by Randomized Phase II Study of SGI-110 With Irinotecan Versus Regorafenib in Previously Treated Metastatic Colorectal Cancer Completed USA | NLD 0
NCT06087263 Phase II Regorafenib Phase 2 Study to Evaluate the Efficacy of Regorafenib in Specific GIST Mutation Subsets (KIT Exon 17, 18, or 14 Mutation and SDHB Deficient GIST) in the Post-imatinib Second-line Setting. Recruiting USA 0
NCT01538680 Phase III Regorafenib Regorafenib in Subjects With Metastatic Colorectal Cancer (CRC) Who Have Progressed After Standard Therapy No longer available USA | SWE | POL | NOR | NLD | ITA | ISR | IRL | HUN | GRC | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CHE | CAN | BEL | AUT | AUS 3
NCT02693535 Phase II Cobimetinib + Vemurafenib Atezolizumab + Talazoparib Regorafenib Larotrectinib Trastuzumab + Tucatinib Ipilimumab + Nivolumab Palbociclib Afatinib Entrectinib Talazoparib Pembrolizumab Temsirolimus Pertuzumab + Trastuzumab Atezolizumab + Pertuzumab/trastuzumab/hyaluronidase-zzxf Crizotinib Abemaciclib Sunitinib Olaparib TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (TAPUR) Recruiting USA 0
NCT04051606 Phase II Regorafenib Phase II Study of Regorafenib in Bevacizumab Refractory Recurrent Glioblastoma Active, not recruiting USA 0
NCT05425940 Phase III Atezolizumab + XL092 Regorafenib Study of XL092 + Atezolizumab vs Regorafenib in Subjects With Metastatic Colorectal Cancer (STELLAR-303) Active, not recruiting USA | POL | NZL | HUN | GBR | FRA | ESP | DEU | BEL | AUS 6
NCT02581059 Phase II Regorafenib Efficacy of Ginseng for Patients on Regorafenib Terminated USA 0
NCT05370807 Phase II Regorafenib A Clinical Trial of Regorafenib in Patients With Pretreated Advanced Melanoma (RegoMel) Recruiting BEL 0
NCT02234180 Phase II Regorafenib Study of Adjuvant Regorafenib vs Placebo in Patients With Node Positive Esophageal Cancer That Completed Pre-operative Therapy Terminated USA 0
NCT02316340 Phase II Vorinostat Hydroxychloroquine Regorafenib Vorinostat Plus Hydroxychloroquine Versus Regorafenib in Colorectal Cancer Completed USA 0
NCT02053376 Phase II Regorafenib A Phase 2 Trial of Regorafenib as A Single Agent in Advanced and Metastatic Biliary Tract Carcinoma/Cholangiocarcinoma Patients Who Have Failed First-line Chemotherapy Completed USA 0
NCT01939223 Phase III Regorafenib COlorectal Cancer Treated With Adjuvant Regorafenib Versus Placebo After Curative Treatment of Liver Metastases in a Randomized, Double-blind, Placebo?Controlled Phase-III STudy (COAST) Terminated USA | ITA | ISR | GBR | FRA | ESP | DEU | CAN | BRA | BEL | AUS 3
NCT06275919 Phase II Regorafenib Regorafenib for Recurrent Grade 2 and 3 Meningioma (MIRAGE Trial) (MIRAGE) Recruiting ITA 0
NCT01103323 Phase III Regorafenib Patients With Metastatic Colorectal Cancer Treated With Regorafenib or Placebo After Failure of Standard Therapy Completed USA | TUR | NLD | ITA | ISR | HUN | FRA | ESP | DEU | CHE | CAN | BRA | BEL | AUS | ARG 4
NCT02795156 Phase II Cabozantinib Afatinib Regorafenib Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations Completed USA 0
NCT04117945 Phase II Regorafenib Irinotecan + Panitumumab Panitumumab Cetuximab + Irinotecan Cetuximab Regorafenib, With Cetuximab or Panitumumab, for the Treatment of Unresectable, Locally Advanced, or Metastatic Colorectal Cancer Active, not recruiting USA 0
NCT02098538 Phase II Regorafenib Regorafenib in Patients With Progressive, Recurrent/Metastatic Adenoid Cystic Carcinoma Completed USA 0
NCT02638766 Phase II Regorafenib Single Agent Regorafenib in First-line for Metastatic/Unresectable KIT/PDGFR Wild Type GIST (REGISTRI) Completed ITA | FRA | ESP 0
NCT02023333 Phase II Regorafenib Regorafenib in Good Performance Status Patients With Newly Diagnosed Metastatic Colorectal Adenocarcinoma Active, not recruiting USA 0
NCT03377361 Phase Ib/II Regorafenib Ipilimumab + Nivolumab + Trametinib Nivolumab + Trametinib An Investigational Immuno-therapy Study Of Nivolumab In Combination With Trametinib With Or Without Ipilimumab In Participants With Previously Treated Cancer of the Colon or Rectum That Has Spread (CheckMate 9N9) Active, not recruiting USA | ITA | ESP | DEU | CZE | CAN | BEL | AUS | ARG 1
NCT05395741 Phase Ib/II Regorafenib Regorafenib in Patients With Refractory Primary Bone Tumors (Regbone) Recruiting POL 0
NCT02466009 Phase II Regorafenib Regorafenib in Metastatic Colorectal Cancer Completed USA 0
NCT03970447 Phase II Lomustine Regorafenib Temozolomide A Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma (GBM AGILE) Recruiting USA | FRA | DEU | CHE | CAN | AUS 0
NCT03563157 Phase Ib/II Aldoxorubicin + Avelumab + Capecitabine + Cetuximab + Cyclophosphamide + ETBX-011 + ETBX-021 + ETBX-051 + ETBX-061 + Fluorouracil + GI-4000 + GI-6207 + GI-6301 + haNK cells + Leucovorin + Nab-paclitaxel + Nogapendekin alfa inbakicept + Oxaliplatin + Regorafenib + Trastuzumab Regorafenib QUILT 3.071: NANT Colorectal Cancer (CRC) Vaccine Active, not recruiting USA 0
NCT05159245 Phase II Vemurafenib Tepotinib Vismodegib Apalutamide Alectinib Regorafenib Entrectinib Pertuzumab + Trastuzumab Pemigatinib Atezolizumab Cobimetinib Dabrafenib + Trametinib Dabrafenib Trametinib Abemaciclib The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs (FINPROVE) Recruiting FIN 0
NCT03844620 Phase II Regorafenib Trifluridine-tipiracil hydrochloride Regorafenib + Trifluridine-tipiracil hydrochloride Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer Active, not recruiting USA 0
NCT02080260 Phase II Regorafenib A Study of Regorafenib in Advanced Pancreatic Cancer Patients Completed USA 0
NCT02439723 Phase I Regorafenib Effects of LBM and PPIs on Pharmacokinetics and Safety of Regorafenib (BAY 73-4506) in Cancer Patients Withdrawn CAN 0
NCT02459119 Phase II Regorafenib Study of Regorafenib for Urothelial Cancer Following Chemotherapy (UAB 1477) Completed USA 0
NCT02096354 Phase II Regorafenib A Phase 2 Randomized, Open-Label Study of RRx-001 vs Regorafenib in Subjects With Metastatic Colorectal Cancer Completed USA 0
NCT02287727 Phase II Regorafenib Regorafenib in Reducing Recurrence in Patients With Non-metastatic Rectal Cancer Who Have Completed Curative-Intent Treatment Withdrawn USA 0
NCT02788279 Phase III Atezolizumab Atezolizumab + Cobimetinib Regorafenib A Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma Completed USA | POL | ITA | GBR | ESP | CAN | BEL | AUS 3
NCT03042689 Phase I Regorafenib Study of Regorafenib in Patients With Advanced Myeloid Malignancies Completed USA 0
NCT02259725 Phase II Regorafenib Regorafenib in Treating Patients With Advanced or Metastatic Neuroendocrine Tumors Completed USA 0
NCT02587650 Phase II Ceritinib Capmatinib Regorafenib Entrectinib Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma Terminated USA 0
NCT01853046 Phase I Regorafenib Pharmacokinetics and Safety of Regorafenib (BAY73-4506) in Cancer Subjects With Severe Renal Impairment Completed USA | CAN 0
NCT05366816 Phase II Regorafenib Sunitinib ctDNA-Guided Sunitinib And Regorafenib Therapy for GIST Recruiting USA 0
NCT04476329 Phase II Regorafenib Optimization for Regorafenib in HCC (ReDos HCC) Terminated USA 0
NCT04055220 FDA approved Regorafenib Efficacy and Safety of Regorafenib as Maintenance Therapy After First-line Treatment in Patients With Bone Sarcomas (REGOSTA) Recruiting FRA 0
NCT02119676 Phase II Regorafenib Ruxolitinib Study of Ruxolitinib in Colorectal Cancer Patients Terminated USA | ISR | GBR | FRA | ESP | DEU | AUS 1
NCT02402036 Phase II Regorafenib A Biomarker Study in Patients Getting Regorafenib for Metastatic Colorectal Cancer Terminated USA 0
NCT02278783 Phase II Regorafenib Phase 2 Trial of Regorafenib in Patients With Recurrent Ovarian, Primary Peritoneal and Fallopian Tube Cancer Terminated USA 0
NCT02466802 Phase I Regorafenib Sildenafil Study of Regorafenib and Sildenafil for Advanced Solid Tumors Completed USA 0
NCT01949194 Phase II Regorafenib Study to Determine the Efficacy of Regorafenib in Metastatic Colorectal Cancer Patients and to Discover Biomarkers Unknown status CAN 0
NCT03793361 Phase II Regorafenib Phase II Study of Regorafenib as Maintenance Therapy Active, not recruiting FRA 0
NCT02241720 Phase II Regorafenib Regorafenib Second Line Treatment of Metastatic or Advanced Upper GI Cancers Terminated USA 0
NCT04327700 Phase II Regorafenib Study Of Intrabucally Administered Electromagnetic Fields and Regorafenib Terminated USA 0
NCT06246643 Phase II Regorafenib A Study of Continued Treatment With Regorafenib in Participants With Solid Tumors Who Have Participated in Other Bayer Studies Active, not recruiting FRA | ESP 3
NCT02048371 Phase II Regorafenib A Blanket Protocol to Study Oral Regorafenib in Patients With Refractory Liposarcoma, Osteogenic Sarcoma, and Ewing/Ewing-like Sarcomas Completed USA 0
NCT02425683 Phase II Regorafenib Study of Colorectal Cancer Patients (Stage IIIC) With Either Regorafenib or Standard of Care (No Treatment) After Adjuvant FOLFOX Terminated USA 0
NCT02389244 Phase II Regorafenib A Phase II Study Evaluating Efficacy and Safety of Regorafenib in Patients With Metastatic Bone Sarcomas (REGOBONE) Recruiting FRA 0
NCT02287025 FDA approved Regorafenib A Phase 4 Study of Regorafenib in Metastatic Colorectal Cancer - Does Educating Physicians Change Patient Out Comes? Terminated USA 0
NCT04787341 Phase II Regorafenib Panitumumab PAnitumumab REchallenge Followed by REgorafenib Versus the Reverse Sequence (PARERE) Recruiting ITA 0
NCT02048722 Phase II Regorafenib Daily Oral Regorafenib for Chemotherapy-Refractory, Metastatic and Locally Advanced Angiosarcoma Completed USA 0
NCT03627728 Phase II Regorafenib Study Maintenance Regorafenib vs Placebo, no Progression Patients After I Line Chemotherapy Metastatic Gastric Cancer (a-MANTRA) Unknown status ITA 0
NCT02773524 Phase III Regorafenib A Study of Regorafenib in Refractory Advanced Gastro-Oesophageal Cancer (INTEGRATEII) Unknown status USA | NZL | CAN | AUS 3
NCT02934529 Phase III Cetuximab + Fluorouracil + Irinotecan + Leucovorin Bevacizumab + Capecitabine + Fluorouracil + Leucovorin Regorafenib Metastatic Colorectal Cancer (RAS-wildtype) After Response to First-line Treatment With FOLFIR Plus Cetuximab (AIO-KRK-0114) Active, not recruiting DEU 0
NCT05622136 Phase II Regorafenib Dose-escalation of Regorafenib in Advanced Hepatocellular Carcinoma (STRAT-aHCC) Recruiting BRA 0
NCT02657551 Phase II Regorafenib A Study Using Regorafenib as Second or Third Line Therapy in Metastatic Medullary Thyroid Cancer Active, not recruiting USA 0
NCT04776148 Phase III Regorafenib Trifluridine-tipiracil hydrochloride Lenvatinib + Pembrolizumab Study of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017) Completed USA | TUR | ISR | GBR | ESP | DNK | DEU | CAN | AUS | ARG 5
NCT02195011 Phase II Regorafenib Safety Study of Regorafenib and SIR-Spheres® Microspheres Radioembolization in Patients With Refractory Metastatic Colorectal Cancer With Liver Metastases Completed USA 0
NCT02115542 Phase II Regorafenib Single Agent Regorafenib in Refractory Advanced Biliary Cancers Completed USA 0
NCT03465722 Phase III Regorafenib Avapritinib (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST Completed USA | SWE | POL | NLD | ITA | HUN | GBR | FRA | ESP | DEU | CZE | CAN | BEL | AUT | AUS 3
NCT03829462 Phase III Regorafenib Irinotecan + Regorafenib Assessing a Regorafenib-irinotecan Combination Versus Regorafenib Alone in Metastatic Colorectal Cancer Patients (NEXT-REGIRI) Active, not recruiting FRA 0
NCT04874207 FDA approved Regorafenib Evaluation of Treatment PERSOnalization Based on Its Therapeutic Monitoring in Patients With Metastatic Colorectal Cancer Treated With REgorafenib (RePERSO) Active, not recruiting FRA 0
NCT04698785 Phase II Regorafenib Efficacy of Regorafenib Combined With Best Supportive Care as Maintenance Treatment in High Grade Bone Sarcomas Patients (REGOMAIN) Recruiting FRA 0
NCT03992456 Phase II Panitumumab Regorafenib Trifluridine-tipiracil hydrochloride Panitumumab, Regorafenib, or TAS-102, in Treating Patients With Metastatic and/or Unresectable RAS Wild-Type Colorectal Cancer Active, not recruiting USA 0
NCT04660812 Phase Ib/II AB680 + Etrumadenant + Zimberelimab Regorafenib Bevacizumab + Etrumadenant + Fluorouracil + Leucovorin + Oxaliplatin + Zimberelimab Etrumadenant + Fluorouracil + Leucovorin + Oxaliplatin + Zimberelimab Bevacizumab + Fluorouracil + Leucovorin + Oxaliplatin An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer. Active, not recruiting USA | ITA | GBR | FRA | ESP 1
NCT02164240 Phase I Sunitinib Regorafenib Phase Ib Study of SUnitinib Alternating With REgorafenib in Patients With Metastatic and/or Unresectable GIST Completed USA 0
NCT01774344 Phase III Regorafenib Study of Regorafenib After Sorafenib in Patients With Hepatocellular Carcinoma (RESORCE) Completed USA | NLD | ITA | HUN | GBR | FRA | ESP | DEU | CZE | CHE | BRA | BEL | AUT | AUS | ARG 6
NCT01298570 Phase II Fluorouracil + Irinotecan + Leucovorin Regorafenib Regorafenib+FOLFIRI Versus Placebo+FOLFIRI as 2nd Line Tx in Metastatic Colorectal Cancer Completed USA | IRL 0
NCT02664077 Phase III Regorafenib A Study Evaluating Regorafenib Following Completion of Standard Chemotherapy for Patients With Colon Cancer (ARGO) Terminated USA 0
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
NCT06425133 Phase II Regorafenib Aspirin + Capecitabine + Cyclophosphamide + Regorafenib Regorafenib in Combination With Multimodal Metronomic Chemotherapy for Chemo-resistant Metastatic Colorectal Cancers (CARE) Not yet recruiting FRA 0


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