Therapy Detail
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| Therapy Name | Binimetinib + Buparlisib |
| 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). |
| Buparlisib | BKM-120|BKM120 | PI3K Inhibitor (Pan) 40 | Buparlisib (BKM120) specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, and may result in apoptotic activity and inhibition of cell proliferation (PMID: 22188813). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF mutant | melanoma | sensitive | Binimetinib + Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Binimetinib (MEK162) and Buparlisib (BKM120) resulted in improved cell growth inhibition compared to either agent alone in a metastatic melanoma cell line harboring a BRAF mutation in culture (PMID: 27307593). | 27307593 |
| NRAS mutant | melanoma | sensitive | Binimetinib + Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Binimetinib (MEK162) and Buparlisib (BKM120) resulted in improved cell growth inhibition compared to either agent alone in a metastatic melanoma cell line harboring an NRAS mutation (PMID: 27307593). | 27307593 |
| BRAF wild-type NRAS wild-type | melanoma | sensitive | Binimetinib + Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Binimetinib (MEK162) and Buparlisib (BKM120) resulted in improved cell growth inhibition compared to either agent alone in a metastatic melanoma cell line with wild-type BRAF and wild-type NRAS in culture (PMID: 27307593). | 27307593 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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