Dr. med. Dirk Manski

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Abiraterone: Androgen Synthesis Inhibitor for Metastatic Prostate Cancer

Indications for Abiraterone

Castration-Sensitive Metastatic Prostate Carcinoma (M1 CSPC)

Abiraterone is an treatment option for men with high tumor volume of castration-sensitive metastatic prostate cancer. At least 4 bone metastases or the presence of visceral metastases were defined as high tumor volume (Sweeney et al., 2015). The approval of abiraterone was expanded in 2017 based on the results of the STAMPEDE trial (James et al., 2017) and LATITUDE trial (Fizazi et al., 2017). The combination ofstandard androgen deprivation therapy with abiraterone 1000 mg/d and prednisolone 5 mg/d resulted in improved survival (83% vs. 76%), prolonged progression-free survival and prolonged time to chemotherapy.

Castration-Resistant Metastatic Prostate Cancer (M1 CRPC)

Abiraterone is an option to treat men with castration-resistant metastatic prostate cancer before or after chemotherapy. Abiraterone increases survival in patients with CRPC after docetaxel chemotherapy (14.8 vs. 10.9 months) compared to placebo (Bono et al., 2011). Abiraterone also improves prognosis before docetaxel chemotherapy treatment in patients with M1 CRPC: prolonged progression-free survival (16.5 vs. 8.3 months) and overall survival (Ryan et al., 2013).

Abiraterone is not approved for the treatment of increasing PSA levels under classical androgen deprivation therapy and without the detection of metastases in imaging (M0 CRPC).

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 inhibits 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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