Drug intelligence / Profile preview

pembrolizumab + dabrafenib + trametinib

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

Overview

Pembrolizumab + dabrafenib + trametinib is a **combination regimen** used primarily in the treatment of BRAF V600-mutant advanced or metastatic melanoma. **Pembrolizumab** is a monoclonal antibody that inhibits the programmed death 1 (**PD-1**) checkpoint receptor, enhancing anti-tumor immune responses. **Dabrafenib** is a small molecule inhibitor targeting mutant **BRAF** kinase, specifically the V600E/K mutations that drive tumor proliferation. **Trametinib** is a small molecule inhibitor of **MEK1/2**, downstream effectors in the MAPK pathway. This triple therapy aims to combine targeted inhibition of the MAPK pathway through BRAF and MEK blockade with immunomodulation via PD-1 inhibition, resulting in enhanced anti-tumor efficacy compared to conventional doublet therapies. The regimen is in clinical development and use for advanced BRAF V600-mutant melanoma and is also being explored for other BRAF V600E-mutated malignancies[1][2][4][5][6].

Brand names
Keytruda + Tafinlar + Mekinist
Other names
Triple therapy (pembrolizumab, dabrafenib, trametinib)Pembrolizumab in Combination With Dabrafenib and Trametinib
02

Targets

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

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