Drug intelligence / Profile preview

encorafenib + binimetinib + pembrolizumab

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

Overview

This is an investigational combination therapy composed of **encorafenib** (a small molecule BRAF inhibitor), **binimetinib** (a small molecule MEK inhibitor), and **pembrolizumab** (a monoclonal antibody checkpoint inhibitor targeting PD-1). The combination is being evaluated as a first-line treatment for unresectable locally advanced or metastatic melanoma with BRAF V600 mutation. Encorafenib inhibits the activity of BRAF V600-mutant kinase, blocking signalling that promotes cancer cell proliferation[2][3][5][7]. Binimetinib inhibits MEK1/2, further disrupting the RAS/RAF/MEK/ERK pathway[2][3][7]. Pembrolizumab binds to PD-1 on T cells, preventing its interaction with ligands and thus enhancing immune-mediated anti-tumor responses[2]. The triplet regimen is under phase 3 clinical evaluation in the STARBOARD trial, aiming to determine if combining targeted and immunotherapy improves outcomes over monotherapy in BRAF V600-mutant melanoma[2][5][7].

02

Targets

PDCD1 (Programmed cell death protein 1 receptor)BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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