Drug intelligence / Profile preview

vemurafenib + ipilimumab

Development stage
Unknown
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

A dual-therapy regimen combining the small-molecule BRAF inhibitor vemurafenib with the checkpoint inhibitor monoclonal antibody ipilimumab for BRAF-mutated advanced melanoma. Vemurafenib selectively inhibits mutant BRAF (especially V600E/V600K) to suppress MAPK pathway signaling and tumor proliferation, while ipilimumab blocks cytotoxic T-lymphocyte–associated antigen 4 (CTLA-4) to enhance T-cell–mediated antitumor immune responses. Concurrent coadministration was associated with dose-limiting hepatotoxicity in early trials; sequential strategies (vemurafenib lead-in followed by ipilimumab) have shown manageable safety in phase II studies. This combination is investigational and not an approved fixed-combination product.[1][2][10]

Other names
VEM + IPI
02

Targets

CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)BRAF V600E

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