Drug intelligence / Profile preview

androgen deprivation therapy + docetaxel + enzalutamide

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous
01

Overview

A combination regimen consisting of androgen deprivation therapy (ADT), the chemotherapy agent docetaxel, and the next-generation androgen receptor inhibitor enzalutamide. This "triple therapy" is used primarily in the treatment of metastatic castration-sensitive prostate cancer (mCSPC) and metastatic castration-resistant prostate cancer (mCRPC). - **Androgen Deprivation Therapy (ADT):** Suppresses or blocks production of male sex hormones to slow or stop growth of prostate cancer cells. - **Docetaxel:** A taxane-class cytotoxic chemotherapy that disrupts microtubule function, leading to cell cycle arrest and apoptosis in rapidly dividing cells. - **Enzalutamide:** An oral small molecule that inhibits the androgen receptor by blocking binding of androgens, preventing nuclear translocation, and interfering with DNA association. The rationale for this combination is to intensify first-line treatment by targeting both hormone signaling pathways and directly killing tumor cells. Clinical trials such as ENZAMET have shown improved survival outcomes with this approach compared to standard care[1][4][5]. Enzalutamide also has activity against resistant clones via inhibition of drug efflux pumps implicated in resistance mechanisms[4].

Other names
ADT + docetaxel + enzalutamidetriple therapy for metastatic prostate cancer
02

Targets

MicrotubuleGnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)

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