Therapy Detail
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| Therapy Name | AZD6482 + Binimetinib + Encorafenib + NVP-AEW541 |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| AZD6482 | KIN-193|AZD-6482 | PIK3CB inhibitor 8 PIK3CD inhibitor 27 | AZD6482 inhibits PIK3CB and PIK3CD, preventing the activation of the PI3K signaling pathway and inhibiting tumor cell proliferation, motility, and survival (PMID: 24992874, PMID: 23674493, PMID: 31292159, PMID: 30542720). | |
| 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). |
| Encorafenib | Braftovi | LGX818 | BRAF Inhibitor 25 | Braftovi (encorafenib) is an inhibitor of Raf kinase with selective activity against BRAF V600E, resulting in growth inhibition (PMID: 24864047). Braftovi (encorafenib) is FDA approved for use in combination with Mektovi (binimetinib) in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, and in patients with metastatic non-small cell lung cancer harboring BRAF V600E, and in combination with Erbitux (cetuximab) in patients with metastatic colorectal cancer with BRAF V600E (FDA.gov). |
| NVP-AEW541 | IGF-1R Inhibitor 17 | NVP-AEW541 is a small molecule inhibitor of IGF1R that blocks IGF-I-mediated signaling, therefore inhibits tumor cell growth (PMID: 15050915, PMID: 30718793). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF mut PTEN inact mut | melanoma | sensitive | AZD6482 + Binimetinib + Encorafenib + NVP-AEW541 | Preclinical | Actionable | In a preclinical study, combination treatment consists of AZD6482, Binimetinib (MEK162), Encorafenib (LGX818), and NVP-AEW541 efficiently induced apoptosis in melanoma cell lines harboring BRAF mutations and PTEN inactivating mutations in culture (PMID: 26577700). | 26577700 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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