Dr. med. Dirk Manski



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Abiraterone: Androgen Synthesis Inhibitor for Castration Resistant Prostate Cancer

Indications for Abiraterone

Abiraterone is indicated for the treatment of progressive castration-resistant prostate cancer. Abiraterone is a treatment option before or after chemotherapy with docetaxel. Abiraterone increases survival in patients with CRPC (after docetaxel chemotherapy) (14.8 vs 10.9 months with placebo) (Bono et al., 2011). Abiraterone also improves prognosis if chosen before docetaxel chemotherapy: progression-free survival 16.5 vs. 8.3 months compared to placebo and improvement of overall survival (Ryan et al., 2013).

Mechanism of Action of Abiraterone

Abiraterone is a CYP-17 inhibitor and thus an inhibitor of the testosterone biosynthesis.

Pharmacokinetics of Abiraterone

Taking Abiraterone with meals leads to a massive increase in absorption with up to 17-fold increase in peak concentration, therefore intake with meals must be avoided (see dosage). High distribution volume and high plasma protein binding. Elimination half life 15 h, hepatic metabolism and biliary elimination.

Side Effects of Abiraterone

Interactions with Abiraterone

Abiraterone activates the enzyme CYP2D6, therefore dose reduction or caution with metoprolol, propranolol, desimpramine, haloperidol, risperidone, propafenone, flecanide, codeine, oxycodone and tramadol.

Contraindications for Abiraterone

Dosage of Abiraterone

The dosage of abiraterone is 1000 mg 1-0-0 p.o. Abiraterone must be taken on an empty stomach, no food should be consumed for at least two hours before the dose and for at least one hour after the dose. Abiraterone is prescribed together with Prednisolone 10 mg 1-0-0.

Brand Name of Abiraterone:

Zytiga.







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References

de Bono, J. S.; Logothetis, C. J.; Molina, A.; Fizazi, K.; North, S.; Chu, L.; Chi, K. N.; Jones, R. J.; Goodman, O. B.; Saad, F.; Staffurth, J. N.; Mainwaring, P.; Harland, S.; Flaig, T. W.; Hutson, T. E.; Cheng, T.; Patterson, H.; Hainsworth, J. D.; Ryan, C. J.; Sternberg, C. N.; Ellard, S. L.; Fléchon, A.; Saleh, M.; Scholz, M.; Efstathiou, E.; Zivi, A.; Bianchini, D.; Loriot, Y.; Chieffo, N.; Kheoh, T.; Haqq, C. M.; Scher, H. I. & Investigators, C. O. U. A.
Abiraterone and increased survival in metastatic prostate cancer.
N Engl J Med, 2011, 364, 1995-2005


Ryan, C. J.; Smith, M. R.; de Bono, J. S.; Molina, A.; Logothetis, C. J.; de Souza, P.; Fizazi, K.; Mainwaring, P.; Piulats, J. M.; Ng, S.; Carles, J.; Mulders, P. F. A.; Basch, E.; Small, E. J.; Saad, F.; Schrijvers, D.; Poppel, H. V.; Mukherjee, S. D.; Suttmann, H.; Gerritsen, W. R.; Flaig, T. W.; George, D. J.; Yu, E. Y.; Efstathiou, E.; Pantuck, A.; Winquist, E.; Higano, C. S.; Taplin, M.; Park, Y.; Kheoh, T.; Griffin, T.; Scher, H. I.; Rathkopf, D. E. & Investigators, C. O. U. A.
Abiraterone in metastatic prostate cancer without previous chemotherapy.
N Engl J Med, 2013, 368, 138-148.




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