Drug intelligence / Profile preview

pembrolizumab + enzalutamide + androgen deprivation therapy

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous (for Pembrolizumab), Oral (for Enzalutamide), Subcutaneous Or Intramuscular (for ADT/GnRH Analogs/antagonists), Surgical (for Orchiectomy As A Form Of Adt)
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Overview

A combination regimen of **pembrolizumab** (a monoclonal antibody that inhibits the programmed cell death protein 1, PD-1), **enzalutamide** (a small molecule androgen receptor inhibitor), and **androgen deprivation therapy** (ADT; hormonal therapy aimed at reducing androgen levels, typically via GnRH agonists or antagonists or orchiectomy) used primarily for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Pembrolizumab is an immune checkpoint inhibitor that enhances antitumor immune responses by blocking the PD-1 pathway. Enzalutamide blocks androgen receptor activity, thereby inhibiting androgen-driven tumor cell proliferation. ADT further reduces androgen levels systemically, depriving prostate cancer cells of growth signals. The combination has been investigated in multiple clinical trials for potential additive or synergistic effects, though results to date indicate only limited additional clinical benefit over existing standards of care in mCRPC, with increased toxicity reported[1][2][4][5].

Brand names
KeytrudaXtandi
Other names
PD-1 inhibitor + androgen receptor inhibitor + ADTpembrolizumab + enzalutamide + ADT
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Targets

AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)PDCD1 (Programmed cell death protein 1 receptor)

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