Drug intelligence / Profile preview

pembrolizumab + trametinib

Development stage
Phase 2
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**Pembrolizumab + trametinib** is an investigational combination therapy of two pharmaceutical drugs: **pembrolizumab**, a monoclonal antibody against programmed cell death protein 1 (PD-1), and **trametinib**, a small molecule inhibitor of mitogen-activated protein kinase kinase (MEK1/2). Pembrolizumab functions as an immune checkpoint inhibitor, enhancing anti-tumor immunity by blocking inhibitory signaling that suppresses immune response. Trametinib inhibits MEK1 and MEK2, key enzymes in the MAPK/ERK signaling pathway that drive cell proliferation and survival, especially in tumors with activating mutations (such as BRAF V600E/K). While both drugs are approved individually for advanced melanoma, their combination is under investigation, notably in melanoma either with or without BRAF mutations, as a potential strategy to improve response rates and durability via synergistic antiproliferative and immunomodulatory effects. The combination is being explored in clinical trials, sometimes with additional drugs, but "pembrolizumab + trametinib" has no unique approved brand name as a combination product[1][4][5][6].

Other names
pembrolizumab + trametinib
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PDCD1 (Programmed cell death protein 1 receptor)

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