Drug intelligence / Profile preview

dutasteride + bicalutamide

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

A fixed-therapy combination of the 5-alpha-reductase inhibitor dutasteride and the nonsteroidal antiandrogen bicalutamide, investigated primarily for androgen receptor–driven cancers such as prostate cancer. Dutasteride inhibits type I and II 5-alpha-reductase, lowering dihydrotestosterone (DHT) and thereby reducing the high-affinity androgen that competes with bicalutamide; bicalutamide antagonizes the androgen receptor to block androgen signaling. Randomized and prospective trials have evaluated the combination versus bicalutamide alone in prostate cancer settings, showing similar survival with a non-significant trend toward improved PSA progression with combination therapy, and additional studies have explored the combo in castration-resistant and non-metastatic settings and as part of combined androgen blockade backbones in other salivary duct carcinomas responsive to AR signaling.[1][2][6][7][8]

02

Targets

SRD5A1 (Steroid 5-alpha-reductase type 1)SRD5A2 (Steroid 5-alpha-reductase type II)AR (Adrenergic receptors)

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