Drug intelligence / Profile preview

enzalutamide + docetaxel

Development stage
Phase 3
Lead developer
Astellas Pharma
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (for Enzalutamide), Intravenous (for Docetaxel)
01

Overview

**Enzalutamide + docetaxel** is a combination of two pharmaceutical drugs used primarily for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Enzalutamide is an oral androgen receptor inhibitor that blocks androgen receptor binding, nuclear translocation, and receptor DNA activity, while docetaxel is a chemotherapeutic agent that inhibits cell division by binding to and stabilizing microtubules, leading to mitotic arrest and apoptosis. This combination leverages both the androgen receptor inhibition and microtubule targeting to enhance anti-tumor efficacy, with clinical data demonstrating improved progression-free survival and better pain control compared to docetaxel alone in mCRPC patients, particularly those with prior resistance to androgen receptor pathway inhibitors such as abiraterone and enzalutamide[1][2][3][4][5].

02

Targets

AR (Adrenergic receptors)TUBB (Tubulin (alpha and beta subunits))

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