Abiraterone, Yonsa, Zytiga, Androgen Synthesis Inhibitor

  • Indications
  1. Prostate Cancer (advanced, metastatic, castration resistant)
    1. In combination with a GnRH Agonist or surgical castration
  • Mechanism
  1. Steroid antiandrogen that inhibits the enzyme CYP17, in the Testosterone synthesis pathway
  2. Decreases Testosterone synthesis at the Testes and Adrenal Glands
  • Dosing
  1. Abiraterone 1000 mg orally once daily
    1. Combined with Prednisone 5 mg orally once to twice daily
    2. Decrease dose to 250 mg orally daily in moderate hepatic Impairment (Child-Pugh Class B)
  • Adverse Effects
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy
    1. Women should use reliable Contraception for >=3 weeks after their male partner's last dose
  • Drug Interactions
  1. Strong CYP3A4 Inducers
    1. Avoid with Abiraterone
  2. CYP2D6 Substrates with a narrow Therapeutic Index
    1. Avoid with Abiraterone
  • References
  1. (2022) Presc Lett, Medications to treat Prostate Cancer, Resource #380108