Drug intelligence / Profile preview

bicalutamide + dutasteride + tamoxifen

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three small molecule drugs—bicalutamide, dutasteride, and tamoxifen—each with distinct mechanisms of action. Bicalutamide is a non-steroidal antiandrogen that competitively inhibits androgen binding to the androgen receptor, primarily used in prostate cancer therapy[2][5]. Dutasteride is a dual 5-alpha-reductase inhibitor that blocks the conversion of testosterone to dihydrotestosterone (DHT), reducing intraprostatic DHT levels and tumor growth in prostate cancer[1]. Tamoxifen is a selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to its receptor, used mainly for estrogen receptor-positive breast cancers but also for managing gynecomastia induced by antiandrogens like bicalutamide[4][6][8]. This combination may be considered in advanced or hormone-refractory prostate cancer settings or when managing side effects such as gynecomastia from antiandrogen therapy.

02

Targets

ESR1 (ERα)SRD5A2 (Steroid 5-alpha-reductase type II)SRD5A1 (Steroid 5-alpha-reductase type 1)ESR2 (ERβ)AR (Adrenergic receptors)

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