Therapy Detail
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| Therapy Name | Mirdametinib |
| Synonyms | |
| Therapy Description |
Gomekli (mirdametinib), a derivative of CI-1040, is a pan-MEK inhibitor, which inhibits activation of MAPK/ERK resulting in decreased tumor cell proliferation (PMID: 18952427, PMID: 32147669). Gomekli (mirdametinib) is FDA-approved for use in adult and pediatric patients 2 years and older with neurofibromatosis type 1 who have symptomatic plexiform neurofibromas (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Mirdametinib | Gomekli | PD0325901|PD 0325901|PD-901|PD-0325901 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Gomekli (mirdametinib), a derivative of CI-1040, is a pan-MEK inhibitor, which inhibits activation of MAPK/ERK resulting in decreased tumor cell proliferation (PMID: 18952427, PMID: 32147669). Gomekli (mirdametinib) is FDA-approved for use in adult and pediatric patients 2 years and older with neurofibromatosis type 1 who have symptomatic plexiform neurofibromas (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| KIT W557_K558del | gastrointestinal stromal tumor | sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gomekli (mirdametinib) treatment inhibited Erk phosphorylation and decreased expression of ETV1 and CXCR4 in gastrointestinal stromal tumor cells harboring KIT W557_K558del (PMID: 26936919). | 26936919 |
| NRAS G75_E76insDSAMRDQYMRTG | myelodysplastic/myeloproliferative neoplasm | sensitive | Mirdametinib | Preclinical | Actionable | In a preclinical study, Gomekli (mirdametinib) decreased the accumulation of immature myeloid cells in a zebrafish model of myelodysplastic/myeloproliferative neoplasm harboring NRAS G75_E76insDSAMRDQYMRTG (PMID: 38522505). | 38522505 |
| BRAF V600E MAP2K1 L115P | melanoma | resistant | Mirdametinib | Preclinical | Actionable | In a preclinical study, overexpression of MAP2K1 L115P in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by Gomekli (mirdametinib) in cell culture (PMID: 26267534). | 26267534 |
| BRAF V600E | melanoma | conflicting | Mirdametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma cell line xenograft model harboring BRAF V600E treated with Gomekli (mirdametinib) demonstrated stable tumor growth, but by day 44, growth ensued and thus, demonstrated no benefit (PMID: 27488531). | 27488531 |
| BRAF V600E | melanoma | conflicting | Mirdametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gomekli (mirdametinib) treatment induced cell cycle arrest and inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 25422890). | 25422890 |
| BRAF V600E | melanoma | conflicting | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gomekli (mirdametinib) inhibited growth of melanoma cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| NRAS Q61L | acute myeloid leukemia | predicted - sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gomekli (mirdametinib) treatment induced apoptosis and inhibited proliferation of an acute myeloid leukemia cell line harboring NRAS Q61L in culture (PMID: 28923853). | 28923853 |
| STK11 inact mut | Advanced Solid Tumor | sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the presence of an STK11 loss expression signature, which correlates with STK11 inactivating mutations, was associated with increased sensitivity to Gomekli (mirdametinib) in human tumor cell lines in culture (PMID: 27821489). | 27821489 |
| BRAF V600E | glioblastoma | conflicting | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated a decreased response to treatment with Gomekli (mirdametinib), demonstrating increased viability of CD133 positive cells in culture (PMID: 26573800). | 26573800 |
| BRAF V600E | glioblastoma | conflicting | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gomekli (mirdametinib) inhibited growth of glioblastoma cell lines harboring BRAF V600E in culture (PMID: 38714355). | 38714355 |
| NRAS Q61R | melanoma | sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Gomekli (mirdametinib) treatment induced cell cycle arrest and inhibited growth of melanoma cells harboring NRAS Q61R in culture (PMID: 25422890). | 25422890 |
| BRAF V600E MAP2K1 I103N | melanoma | resistant | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, overexpression of MAP2K1 I103N in melanoma cells harboring BRAF V600E resulted in insensitivity to growth inhibition by Gomekli (mirdametinib) in cell culture (PMID: 26267534). | 26267534 |
| BRAF V600E | colon cancer | sensitive | Mirdametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gomekli (mirdametinib) demonstrated antitumor activity against BRAF V600E colon cancer cell line xenografts (PMID: 16273091). | 16273091 |
| BRAF N486_P490del | melanoma | sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF N486_P490del demonstrated sensitivity to Gomekli (mirdametinib), resulting in decreased cell viability in culture (PMID: 26996308). | 26996308 |
| BRAF N486_P490del | ovarian cancer | sensitive | Mirdametinib | Preclinical - Cell culture | Actionable | In a preclinical study, an ovarian cancer cell line harboring BRAF N486_P490del demonstrated sensitivity to Gomekli (mirdametinib), resulting in decreased cell viability in culture (PMID: 26996308). | 26996308 |
| MAP2K1 Q56P | lung adenocarcinoma | sensitive | Mirdametinib | Preclinical | Actionable | In a preclinical study, a lung adenocarcinoma cell line harboring MAP2K1 Q56P demonstrated sensitivity to Gomekli (mirdametinib), resulting in decreased cell viability (PMID: 26582713). | 26582713 |
| BRAF V600E | colorectal cancer | sensitive | Mirdametinib | Preclinical | Actionable | In a preclinical study, Gomekli (mirdametinib) inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture (PMID: 26267534). | 26267534 |
| NRAS mutant | melanoma | no benefit | Mirdametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gomekli (mirdametinib) treatment resulted in stable tumor growth in melanoma cell line xenograft models harboring an NRAS mutation, however, growth later ensued and thus, demonstrates a lack of benefit (PMID: 27488531). | 27488531 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT01347866 | Phase I | Gedatolisib Mirdametinib Irinotecan | Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer | Terminated | USA | ITA | ESP | CAN | 0 |
| NCT04923126 | Phase Ib/II | Mirdametinib | SJ901: Evaluation of Mirdametinib in Children, Adolescents, and Young Adults With Low-Grade Glioma | Recruiting | USA | 0 |
| NCT03962543 | Phase II | Mirdametinib | MEK Inhibitor Mirdametinib (PD-0325901) in Patients With Neurofibromatosis Type 1 Associated Plexiform Neurofibromas (ReNeu) | Active, not recruiting | USA | 0 |
| NCT02096471 | Phase II | Mirdametinib | MEK Inhibitor PD-0325901 Trial in Adolescents and Adults With NF1 | Completed | USA | 0 |
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