Drug intelligence / Profile preview

pembrolizumab + enzalutamide

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

Overview

**Pembrolizumab + enzalutamide** is an experimental drug combination for metastatic castration-resistant prostate cancer (mCRPC). **Pembrolizumab** is a monoclonal antibody that selectively binds to the programmed cell death protein 1 (PD-1) receptor, blocking the interaction with its ligands (PD-L1 and PD-L2) and enhancing T-cell–mediated antitumor immune responses. **Enzalutamide** is an androgen receptor inhibitor that prevents androgens from binding to the androgen receptor and inhibits androgen receptor nuclear translocation and DNA binding, suppressing androgen signaling in prostate cancer cells. Multiple clinical trials (including Phase II and III KEYNOTE-365, KEYNOTE-641, and KEYNOTE-199) have evaluated the efficacy and safety of this combination in patients with mCRPC, usually after progression or intolerance to abiraterone and in the pre-chemotherapy setting. Results indicate the combination is generally manageable in terms of adverse events, with modest or limited antitumor activity and no significant improvement in survival compared to enzalutamide alone in randomized Phase III trials[1][2][3][4][5][6].

02

Targets

AR (Adrenergic receptors)PDCD1 (Programmed cell death protein 1 receptor)

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