Therapy Detail
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| Therapy Name | Binimetinib + Imatinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Binimetinib | Mektovi | ARRY-162|ARRY-438162|MEK162 | MEK inhibitor (Pan) 24 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mektovi (binimetinib) inhibits MEK1 and MEK2 resulting in inhibition of growth factor-mediated signaling and decreased tumor cell proliferation (PMID: 23587417). Mektovi (binimetinib) in combination with Braftovi (encorafenib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov). |
| Imatinib | Gleevec | CGP-57148B|STI571|Imatinib mesylate | ABL Inhibitor (pan) 9 BCR-ABL Inhibitor 31 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). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| KIT W557_K558del KIT N822K | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT N822K was identified as a secondary resistance mutation in a patient with a gastrointestinal stromal tumor harboring a primary KIT W557_K558del mutation who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) (PMID: 35041493; NCT01991379). | 35041493 |
| KIT V560D KIT D820G KIT N822K KIT Y870* | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT N822K and KIT D820G were identified as secondary resistance mutations in a patient with a gastrointestinal stromal tumor harboring primary KIT Y870* and V560D mutations who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) treatment (PMID: 35041493; NCT01991379). | 35041493 |
| KIT Q556_V559delinsHT KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT V654A was identified as a secondary resistance mutation in a patient with a gastrointestinal stromal tumor harboring a primary KIT Q556_V559delinsHT mutation who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) (PMID: 35041493; NCT01991379). | 35041493 |
| KIT E562_L576del | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment resulted in an 80% pathological response and 23% RECIST response in a patient with a small bowel gastrointestinal stromal tumor harboring KIT E562_L576del (PMID: 35041493; NCT01991379). | 35041493 |
| KIT V560D | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment had manageable toxicity and resulted in a 95% pathological response and 6% RECIST response in a patient with gastrointestinal stromal tumor of the stomach harboring KIT V560D (PMID: 35041493; NCT01991379). | 35041493 |
| KIT E554_K558del | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment had manageable toxicity and resulted in a 99% pathological response and 29% RECIST response in a patient with a rectal gastrointestinal stromal tumor harboring KIT E554_K558del (PMID: 35041493; NCT01991379). | 35041493 |
| KIT E562_L576del KIT N822Y | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT N822Y was identified as a secondary mutation in a patient with a gastrointestinal stromal tumor harboring a primary KIT E562_L576del mutation who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) (PMID: 35041493; NCT01991379). | 35041493 |
| KIT E554_K558del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT V654A was identified as a secondary resistance mutation in a patient with a gastrointestinal stromal tumor harboring a primary KIT E554_K558del mutation who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) treatment (PMID: 35041493; NCT01991379). | 35041493 |
| KIT V560del | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Preclinical | Actionable | In a preclinical study, combination treatment with Gleevec (imatinib) and Mektovi (binimetinib) resulted in greater inhibition of tumor growth than either agent alone in a mouse model of gastrointestinal stromal tumor harboring KIT V558del (corresponding to V560del in human) (PMID: 25572173). | 25572173 |
| KIT K558_V559del | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment resulted in a 70% pathological response and 46% RECIST response in a patient with a rectal gastrointestinal stromal tumor harboring KIT K558_V559del (PMID: 35041493; NCT01991379). | 35041493 |
| KIT Q556_I571del KIT V654A | gastrointestinal stromal tumor | predicted - resistant | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, KIT V654A was identified as a secondary mutation in a patient with a gastrointestinal stromal tumor harboring a primary KIT Q556_I571del mutation who developed resistance to Gleevec (imatinib) and Mektovi (binimetinib) (PMID: 35041493; NCT01991379). | 35041493 |
| KIT A502_Y503dup | gastrointestinal stromal tumor | predicted - sensitive | Binimetinib + Imatinib | Case Reports/Case Series | Actionable | In a Phase II trial, Gleevec (imatinib) and Mektovi (binimetinib) combination treatment resulted in a 90% pathological response and 27% RECIST response in the primary tumor and 100% pathological response in metastatic lesions of a patient with an esophageal gastrointestinal stromal tumor harboring KIT A502_Y503dup (PMID: 35041493; NCT01991379). | 35041493 |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04598009 | Phase II | Binimetinib + Imatinib | Binimetinib and Imatinib for Unresectable Stage III-IV KIT-Mutant Melanoma | Recruiting | USA | 0 |
| NCT01991379 | Phase Ib/II | Binimetinib + Imatinib | MEK162 in Combination With Imatinib Mesylate in Patients With Untreated Advanced Gastrointestinal Stromal Tumor (GIST) | Active, not recruiting | USA | 0 |
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