Therapy Detail
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| Therapy Name | Binimetinib + CHZ868 |
| 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) 26 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). |
| CHZ868 | JAK2 Inhibitor 19 | CHZ868 is a type II JAK2 inhibitor, which stabilizes JAK2 in the inactive conformation resulting in decreased downstream signaling and potentially leading to decreased tumor cell growth (PMID: 26175413, PMID: 30498775). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| JAK2 V617F | polycythemia vera | sensitive | Binimetinib + CHZ868 | Preclinical | Actionable | In a preclinical study, CHZ868 and Mektovi (binimetinib) combination treatment decreased splenomegaly, reticulocytes, hematocrit, and allele burden, and reduced expansion of progenitor cells, an effect not observed with treatment of either agent alone, in a mouse model of polycythemia vera harboring JAK2 V617F (PMID: 30730307). | 30730307 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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