Drug intelligence / Profile preview

abiraterone + dutasteride

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral
01

Overview

Abiraterone + dutasteride is a combination therapy consisting of abiraterone, a selective inhibitor of CYP17A1 (17α-hydroxylase/C17,20-lyase), and dutasteride, a dual 5α-reductase inhibitor. Abiraterone blocks androgen biosynthesis by inhibiting CYP17A1, reducing the production of testosterone and other androgens that drive prostate cancer growth. Dutasteride inhibits both type 1 and type 2 isoforms of 5α-reductase, preventing the conversion of testosterone to dihydrotestosterone (DHT) as well as blocking the formation of certain abiraterone metabolites that may act as androgen receptor agonists. The combination aims to enhance antitumor activity in castration-resistant prostate cancer (CRPC) by further suppressing intratumoral androgen signaling and overcoming resistance mechanisms related to abiraterone metabolism[1][2][3][6]. Clinical studies have shown promising PSA response rates in patients with CRPC who are naïve or resistant to second-generation antiandrogens or chemotherapy[1][2][3].

02

Targets

3β-HSD (3β-Hydroxysteroid Dehydrogenase/Δ5-4 isomerase type 1)AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CYP21A2 (Cytochrome P450 21-hydroxylase)SRD5A1 (Steroid 5-alpha-reductase type 1)SRD5A2 (Steroid 5-alpha-reductase type II)

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