Drug intelligence / Profile preview

bicalutamide

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

Overview

Bicalutamide is a nonsteroidal antiandrogen used primarily in the treatment of prostate cancer, especially metastatic prostate cancer. It acts as an androgen receptor antagonist, blocking the effects of androgens (male hormones) such as testosterone by competitively inhibiting their binding to the androgen receptor. This inhibition prevents androgens from stimulating the growth of normal and malignant prostatic tissue, thereby slowing or stopping tumor progression[1][3][4][5]. Bicalutamide is typically administered orally in combination with a gonadotropin-releasing hormone (GnRH) analogue or following surgical castration. While its main indication is for advanced prostate cancer, it has also been used off-label for conditions like excessive hair growth in women, scalp hair loss, puberty blocking in transgender girls and women, gonadotropin-independent early puberty in boys, and prevention of priapism[5]. The drug was developed as a racemic mixture containing both (R)-bicalutamide (active) and (S)-bicalutamide enantiomers[4].

Brand names
Casodex
Other names
bicalutamidebicalutamidabicalutamidumracemic bicalutamideBICALUTAMIDE [USP-RS]BICALUTAMIDE [EP MONOGRAPH]BICALUTAMIDE [ORANGE BOOK]N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide(+-)-bicalutamideNSC-759816NSC759816NSC 759816NSC722665NSC-722665NSC 7226654'-cyano-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methyl-3'-(trifluoromethyl)propionanilide
02

Targets

AR (Adrenergic receptors)

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