Bicalutamide (DB01128): A Comprehensive Monograph on its Pharmacology, Clinical Applications, and Safety Profile

Executive Summary

Bicalutamide is a second-generation, orally active, nonsteroidal antiandrogen (NSAA) primarily utilized in the management of prostate cancer. As a pure and selective antagonist of the androgen receptor (AR), its mechanism of action involves the competitive inhibition of androgen binding, thereby preventing the hormonal stimulation that drives the growth of androgen-dependent tissues. This report provides a comprehensive analysis of Bicalutamide, encompassing its physicochemical properties, detailed pharmacology, clinical applications, safety profile, and regulatory history.

The drug is formulated as a racemate, with its therapeutic activity residing almost exclusively in the (R)-enantiomer, which possesses a long elimination half-life of approximately one week, permitting a convenient once-daily dosing regimen. In oncology, Bicalutamide is principally indicated at a dose of 50 mg/day as a component of combined androgen blockade (CAB) with a gonadotropin-releasing hormone (GnRH) analogue for the treatment of metastatic prostate cancer. A higher dose of 150 mg/day as monotherapy is approved in the European Union and other regions for locally advanced prostate cancer, offering a quality-of-life advantage over castration by preserving bone mineral density and sexual function, though this indication is not approved in the United States.