Drug intelligence / Profile preview

abiraterone + enzalutamide + docetaxel

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of abiraterone, enzalutamide, and docetaxel is an investigational triplet therapy used in treating metastatic castration-resistant prostate cancer (mCRPC). **Abiraterone** is a selective and irreversible inhibitor of CYP17A, a key enzyme in androgen biosynthesis, leading to decreased androgen levels. **Enzalutamide** is a potent androgen receptor (AR) signaling inhibitor, blocking AR binding, nuclear translocation, and DNA transcription activation. **Docetaxel** is a microtubule inhibitor classified as a taxane chemotherapy, which inhibits mitosis by stabilizing microtubules and disrupting cell division. This triplet therapy targets both androgen signaling and cell division, aiming for synergistic antitumor effects in advanced prostate cancer. There is evidence for clinical benefit of adding abiraterone or enzalutamide to docetaxel, with improved outcomes in progression-free survival and metastasis response, and manageable toxicity profiles. However, significant cross-resistance may limit sequential and concurrent efficacy, and triple-regimen studies remain ongoing[2][3][4][6].

02

Targets

MicrotubuleCYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)AR (Adrenergic receptors)

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