Drug intelligence / Profile preview

encorafenib + cetuximab + pembrolizumab

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

Overview

This is a **combination regimen** consisting of three agents: the BRAF inhibitor **encorafenib**, the EGFR monoclonal antibody **cetuximab**, and the PD-1 checkpoint inhibitor **pembrolizumab**. Encorafenib acts as a selective inhibitor of the mutant BRAF V600E protein, disrupting the MAPK/ERK signaling pathway in tumor cells. Cetuximab is a chimeric monoclonal antibody that targets the epidermal growth factor receptor (EGFR), blocking downstream signaling that supports tumor growth and survival. Pembrolizumab is a humanized monoclonal antibody against programmed cell death protein 1 (PD-1), promoting anti-tumor immune responses by inhibiting immune checkpoint signaling. This combination is being investigated in the SEAMARK Phase II study for use as a first-line therapy in patients with previously untreated metastatic colorectal cancer (mCRC) harboring both BRAF V600E mutations and microsatellite instability-high (MSI-H)/mismatch repair-deficient (dMMR) phenotypes[1][2][6].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)PDCD1 (Programmed cell death protein 1 receptor)BRAF V600E

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