Biluron 50 Mechanism of Action

Pharmacotherapeutic Group: Antiandrogen. ATC code: L02 B B03.
Pharmacology: Pharmacodynamics: Bicalutamide is a non-steroidal anti-androgen, devoid of other endocrine activity. It binds to androgen receptors without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours result from this inhibition. Clinically discontinuation of Bicalutamide can result in antiandrogen withdrawal syndrome in a subset of patients. Bicalutamide is a racemate with its antiandrogenic activity being almost exclusively in the (R)-enantiomer.
Pharmacokinetics: The pharmacokinetics parameters of 68 subjects (72 subjects were included in the study, and 69 completed the study, 1 subject was dropped before analyses to keep the study balanced) were calculated and results were statistically analyzed to demonstrate bioequivalence in a one period parallel bioequivalence study. After oral administration of Bicalutamide 50 mg film coated tablets (test product) the mean of the maximum plasma concentration (C_max) (rate of absorption) was 913.0 ng/mL. The median T_max was 33.95 h. The extent of absorption is expressed in Area Under the Curve (AUC)_0-72 and AUC_0-inf the mean values were 176329.8 ng·h/mL and 183372.6 ng·h/mL respectively. The mean elimination half life (T_¹/2) of Bicalutamide 50 mg film coated tablets was 120.51 h.
The ratios and confidence intervals between test and reference product were as following: for C_max the ratio was 94.39% (88.20%-101.01%). For AUC_0-72 the ratio was 93.42% (84.01%-103.89%). The results of the study showed that the ratios and confidence intervals are within the acceptance range for bioequivalence, therefore it can be concluded that the test product, Bicalutamide 50 mg film coated tablets, is bioequivalence with the reference product.