Pharm

Abiraterone

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Abiraterone, Yonsa, Zytiga, Androgen Synthesis Inhibitor

  • See Also
  1. Hormonally Active Chemotherapy
  2. 5a-Reductase 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
  1. Cardiovascular
    1. Fluid retention
    2. Hypertension
    3. QTc Prolongation
    4. Hypertriglyceridemia or Hyperlipidemia
  2. Electrolytes
    1. Hypokalemia
  3. Endocrine
    1. Hot Flushes
    2. Hyperglycemia
  4. Gastrointestinal
    1. Hepatotoxicity with increased Liver Function Tests (including Alkaline Phosphatase)
    2. Diarrhea
    3. Vomiting
    4. Dyspepsia
  5. Other
    1. Anemia
    2. Fatigue
    3. Arthralgias
    4. Myalgias
  • 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
  • Resources
  1. Abiraterone (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4e338e89-3cf2-48eb-b6e2-a06c608c6513
  • References
  1. (2022) Presc Lett, Medications to treat Prostate Cancer, Resource #380108