Drug intelligence / Profile preview

docetaxel + leuprolide + bicalutamide

Development stage
Phase 2
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous, Oral, Subcutaneous
01

Overview

This drug is a **combination therapy** consisting of three approved agents used in the treatment of advanced prostate cancer: - **Docetaxel**: a taxane-class chemotherapy agent that inhibits microtubule depolymerization, thereby disrupting mitosis and inducing tumor cell death. - **Leuprolide**: a gonadotropin-releasing hormone (GnRH) agonist that suppresses androgen production via downregulation of pituitary gonadotropins, leading to chemical castration. - **Bicalutamide**: a nonsteroidal antiandrogen that blocks activation of the androgen receptor by competing with testosterone and dihydrotestosterone, inhibiting androgen-dependent tumor growth. This combination is used primarily as part of **androgen deprivation therapy (ADT) plus chemotherapy** for patients with advanced, high-risk, or metastatic prostate cancer. The rationale is to maximally suppress androgen signaling (with leuprolide and bicalutamide) and to directly kill rapidly dividing tumor cells (with docetaxel). Clinical evidence supports the benefit of the combined approach versus monotherapy in controlling disease progression, lowering PSA, and prolonging survival[1][2][5][6][7].

02

Targets

AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)TUBB (Tubulin (alpha and beta subunits))

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