Therapy Detail
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| Therapy Name | MK2206 + Vemurafenib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| MK2206 | MK-2206|MK 2206 | Akt Inhibitor (Pan) 21 | MK2206 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway and tumor cell proliferation (PMID: 20571069, PMID: 32194695). | |
| Vemurafenib | Zelboraf | RO5185426|PLX4032 | RAF Inhibitor (Pan) 28 | Zelboraf (vemurafenib) inhibits BRAF V600E, wild-type BRAF, ARAF, and CRAF (PMID: 20179705), which may result in an inhibition of the MAPK signaling pathway resulting in a reduction of tumor cell proliferation (PMID: 20823850). Zelboraf (vemurafenib) is FDA approved for BRAF V600E-mutant melanoma and for BRAF V600-positive Erdheim-Chester disease (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E PIK3CA H1047R | colorectal cancer | sensitive | MK2206 + Vemurafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zelboraf (vemurafenib) treatment in combination with MK2206 induced apoptosis and synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 22180495). | 22180495 |
| BRAF V600X | melanoma | sensitive | MK2206 + Vemurafenib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of MK2206 and Zelboraf (vemurafenib) inhibited growth of BRAF V600-mutant melanoma cell lines in culture, with increased efficacy over either agent alone (PMID: 24265152). | 24265152 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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