99% Content Bicalutamide CAS 90357-06-5 Anti-Prostate Cancer Drug

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Description

Bicalutamide is a member of the nonsteroidal antiandrogen (NSAA) group of medications. It works by blocking the androgen receptor (AR), the biological target of the androgen sex hormones testosterone and dihydrotestosterone (DHT). It does not lower androgen levels.[6] The medication can have some estrogen-like effects in men. Bicalutamide is well-absorbed, and its absorption is not affected by food. The terminal half-life of the medication is around one week. It is believed to cross the blood-brain barrier and affect both the body and brain.

Bicalutamid has a molecular weight of 430.37. The pKa' is approximately 12. Bicalutamid is a fine white to off white powder which is practically insoluble in water at 37°C (5 mg per 1000 mL), slightly soluble in chloroform and absolute ethanol, sparingly soluble in methanol, and soluble in acetone and tetrahydrofuran.CASODEX (bicalutamid) is a racemate with its antiandrogenic activity being almost exclusively exhibited by the R-enantiomer of bicalutamid; the S-enantiomer is essentially inactive.


Application

Bicalutamid is used primarily in the treatment of early and advanced prostate cancer. It is approved at a dosage of 50 mg/day as a combination therapy with a gonadotropin-releasing hormone (GnRH) analogue or orchiectomy (that is, surgical or medical castration) in the treatment of stage D2 metastatic prostate cancer (mPC), and as a monotherapy at a dosage of 150 mg/day for the treatment of stage C or D1 locally advanced prostate cancer (LAPC). Although effective in mPC and LAPC, bicalutamid is no longer indicated for the treatment of localized prostate cancer (LPC) due to negative findings in the Early Prostate Cancer (EPC) trial.