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Therapy Name | Vemurafenib + ZSTK474 |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
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). |
ZSTK474 | ZSTK-474 | PI3K Inhibitor (Pan) 41 | ZSTK474 is a pan-PI3K inhibitor, which blocks PI3K/AKT signaling to prevent cell growth (PMID: 16622124, PMID: 30205797). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF V600E/K PIK3CA wild-type | melanoma | sensitive | Vemurafenib + ZSTK474 | Preclinical | Actionable | In a preclinical study, ZSTK474 and Zelboraf (vemurafenib) worked synergistically to inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). | 26137449 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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