Therapy Detail

Therapy Name Pexidartinib + Vemurafenib
Synonym
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Pexidartinib PLX3397 CSF1R Inhibitor 22 FLT3 Inhibitor 50 KIT Inhibitor 48 Pexidartinib (PLX3397) inhibits multiple receptor tyrosine kinases, including KIT, CSF1R, FLT3, and FLT3/ITD, which may inhibit growth in cancer cells (PMID: 22294205, PMID: 25993548, PMID: 25847190).
Vemurafenib Zelboraf RO5185426|PLX4032 RAF Inhibitor (Pan) 17 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E CSF1R positive melanoma sensitive Pexidartinib + Vemurafenib Preclinical Actionable In a preclinical study, a melanoma mouse model harboring BRAF V600E treated with Zelboraf (vemurafenib) demonstrated a greater drug induced sensitivity when treatment was combined with PLX3397, resulting in increased infiltration of lymphocytes via Csf1r inhibition and elevated antitumor activity (PMID: 25939769). 25939769
Clinical Trial Phase Therapies Title Recruitment Status
NCT01826448 Phase I Pexidartinib + Vemurafenib A Phase 1b Open Label, Dose Escalation Study of PLX3397 in Combination With Vemurafenib in V600-mutated BRAF Melanoma Terminated