Abstract
The non-steroidal antiandrogen drug bicalutamide (BIC) is used in the treatment of prostate cancer. It blocks the stimulatory effects of androgens on the growth of prostate cancer cells by blocking binding to androgen receptors in the prostate gland. BIC is a racemic mixture, and the (R)-enantiomer exhibits the main effect. It has been reported that BIC provides the targeted antiandrogenic effect due to its high selectivity, but its adverse effects should be carefully monitored. (R)-BIC is slowly absorbed after oral administration, and its absorption is dose-dependent. The drug is extensively metabolized in the liver, while elimination is largely achieved by renal and hepatic pathways. BIC and its metabolites are found in almost equal amounts in urine and feces. This review comprehensively covers the physicochemical properties, analytical methods, pharmacokinetics, bioavailability, and pharmacology of BIC.
References
- National Center for Biotechnology Information (2025). PubChem Compound Summary for CID 2375, Bicalutamide. Retrieved April 20, 2025, from https://pubchem.ncbi.nlm.nih.gov/ compound/Bicalutamide. Pacult, J., Rams-Baron, M., Chmiel, K., Jurkiewicz, K., Antosik, A., Szafraniec, J., & Paluch, M. (2019). How can we improve the physical stability of co-amorphous system containing flutamide and bicalutamide? The case of ternary amorphous solid dispersions. European Journal of Pharmaceutical Sciences, 136, 104947. https://doi.org/10.1016/j. ejps.2020.105697
Abstract
Bikalutamid (BIC) prostat kanseri tedavisinde kullanılan steroidal olmayan bir anti-androjen ilaçtır. Prostat bezindeki androjen reseptörlerine bağlanmayı engelleyerek androjenlerin prostat kanseri hücrelerinin büyümesi üzerindeki uyarıcı etkilerini bloke eder. BIC rasemik bir karışımdır ve esas etkiyi (R)-enantiyomeri sergiler. BIC’nin yüksek selektivitesi sayesinde hedeflenen antiandrojenik etkiyi sağladığı, ancak advers etkilerinin dikkatli izlenmesi gerektiği belirtilmiştir. (R)-BIC, oral uygulama sonrası yavaş bir şekilde emilir ve emilimi doza bağlıdır. İlacın metabolizasyonu karaciğerde yoğun olarak gerçekleşirken, eliminasyon büyük ölçüde renal ve hepatik yollarla sağlanır. BIC ve metabolitleri idrar ve dışkıda neredeyse eşit oranda bulunur. Bu derleme BIC’nin fizikokimyasal özellikleri, analitik yöntemleri, farmakokinetiği, biyoyararlanımı ve farmakolojisini kapsamlı bir şekilde ele almıştır.
References
- National Center for Biotechnology Information (2025). PubChem Compound Summary for CID 2375, Bicalutamide. Retrieved April 20, 2025, from https://pubchem.ncbi.nlm.nih.gov/ compound/Bicalutamide. Pacult, J., Rams-Baron, M., Chmiel, K., Jurkiewicz, K., Antosik, A., Szafraniec, J., & Paluch, M. (2019). How can we improve the physical stability of co-amorphous system containing flutamide and bicalutamide? The case of ternary amorphous solid dispersions. European Journal of Pharmaceutical Sciences, 136, 104947. https://doi.org/10.1016/j. ejps.2020.105697
Details
| Primary Language | English |
|---|---|
| Subjects | Pharmaceutical Delivery Technologies, Pharmacology and Pharmaceutical Sciences (Other) |
| Journal Section | Collection |
| Authors | |
| Publication Date | August 26, 2025 |
| Submission Date | January 13, 2025 |
| Acceptance Date | May 27, 2025 |
| Published in Issue | Year 2025 Volume: 50 Issue: 2 |
