Drug intelligence / Profile preview

PF-07799933 + cetuximab

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

Overview

PF-07799933 + cetuximab is an investigational combination therapy for advanced solid tumors, specifically targeting cancers with BRAF mutations. PF-07799933 is an oral, selective, ATP-competitive small-molecule RAF kinase inhibitor that suppresses BRAF signaling in BRAF V600-mutant and non-V600-BRAF mutant tumors, displaying minimal paradoxical activation and sparing non-BRAF-mutated RAF dimers. Cetuximab is a recombinant monoclonal antibody targeting the epidermal growth factor receptor (EGFR), inhibiting ligand binding, receptor activation, and downstream signaling. The combination is being evaluated for synergistic antitumor activity and resistance prevention by concurrently inhibiting BRAF-driven MAPK signaling (via PF-07799933) and EGFR-mediated signaling (via cetuximab), especially in tumors showing resistance to current BRAF inhibitors. The therapy is under clinical investigation for patients who have progressed on prior standard treatments, including previous BRAF inhibitors[1][2][3][4][5].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)BRAF (B-Raf proto-oncogene, serine/threonine kinase)

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