Therapy Detail
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| Therapy Name | Refametinib |
| Synonyms | |
| Therapy Description |
Refametinib (BAY86-9766) is an inhibitor of MEK1 and MEK2, which prevents growth-factor mediated cell proliferation (PMID: 24204195). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Refametinib | BAY 869766|BAY 8697661|BAY-869766|BAY-8697661|BAY86-9766|RDEA-119|RDEA119 | MEK inhibitor (Pan) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 | Refametinib (BAY86-9766) is an inhibitor of MEK1 and MEK2, which prevents growth-factor mediated cell proliferation (PMID: 24204195, PMID: 32314268). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| PIK3CA wild-type | colon cancer | sensitive | Refametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Refametinib (BAY86-9766) treatment inhibited colony formation, and induced cell death and apoptosis in PIK3CA wild-type colon cancer cells in culture (PMID: 30944457). | 30944457 |
| PIK3CA mutant | colon cancer | predicted - resistant | Refametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Refametinib (BAY86-9766) treatment did not induce cell death, apoptosis, or inhibit colony formation in PIK3CA mutant colon cancer cells in culture (PMID: 30944457). | 30944457 |
| BRAF V600E | colorectal cancer | sensitive | Refametinib | Preclinical | Actionable | In a preclinical study, Refametinib (BAY86-9766) inhibited growth of colorectal cancer cell lines harboring BRAF V600E in culture and suppressed tumor growth in cell line xenograft models (PMID: 19706763). | 19706763 |
| CTNNB1 over exp PIK3CA wild-type | colon cancer | resistant | Refametinib | Preclinical - Cell culture | Actionable | In a preclinical study, overexpression of CTNNB1 in PIK3CA wild-type colon cancer cells suppressed cell death following Refametinib (BAY86-9766) treatment in culture (PMID: 30944457). | 30944457 |
| MAP2K1 Q56P | lung adenocarcinoma | sensitive | Refametinib | Preclinical | Actionable | In a preclinical study, a lung adenocarcinoma cell line harboring MAP2K1 Q56P demonstrated sensitivity to Refametinib (BAY86-9766), resulting in decreased cell viability (PMID: 26582713). | 26582713 |
| BRAF V600E | melanoma | sensitive | Refametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Refametinib (BAY86-9766) inhibited growth of melanoma cell lines harboring BRAF V600E in culture and suppressed tumor growth in cell line xenograft models (PMID: 19706763). | 19706763 |
| Unknown unknown | Advanced Solid Tumor | not applicable | Refametinib | Phase I | Actionable | In a Phase I trial, Refametinib (BAY 86-9766) was well-tolerated and displayed some evidence of clinical benefit across several tumor types (PMID: 23434733). | 23434733 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02168777 | Phase Ib/II | Refametinib + Regorafenib Refametinib | Refametinib (BAY86-9766) in Combination With Regorafenib (Stivarga, BAY73-4506) in Patients With Advanced or Metastatic Cancer | Terminated | USA | 0 |
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