II. Indications
-
Prostate Cancer (advanced, metastatic, castration resistant)
- In combination with a GnRH Agonist or surgical castration
III. Mechanism
- Steroid antiandrogen that inhibits the enzyme CYP17, in the Testosterone synthesis pathway
- Decreases Testosterone synthesis at the Testes and Adrenal Glands
IV. Dosing
- Abiraterone 1000 mg orally once daily
- Combined with Prednisone 5 mg orally once to twice daily
- Decrease dose to 250 mg orally daily in moderate hepatic Impairment (Child-Pugh Class B)
V. Adverse Effects
- Cardiovascular
- Fluid retention
- Hypertension
- QTc Prolongation
- Hypertriglyceridemia or Hyperlipidemia
- Electrolytes
- Endocrine
- Gastrointestinal
- Hepatotoxicity with increased Liver Function Tests (including Alkaline Phosphatase)
- Diarrhea
- Vomiting
- Dyspepsia
- Other
- Anemia
- Fatigue
- Arthralgias
- Myalgias
VI. Safety
- Avoid in Lactation
- Avoid in pregnancy
- Women should use reliable Contraception for >=3 weeks after their male partner's last dose
VII. Drug Interactions
- Strong CYP3A4 Inducers
- Avoid with Abiraterone
-
CYP2D6 Substrates with a narrow Therapeutic Index
- Avoid with Abiraterone
VIII. Resources
IX. References
- (2022) Presc Lett, Medications to treat Prostate Cancer, Resource #380108
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Related Studies
abiraterone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ABIRATERONE ACETATE 250 MG TAB | Generic | $1.46 each |
Ontology: abiraterone (C0754011)
Definition (NCI) | A steroidal compound with antiandrogen activity. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex; CYP17A1), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. |
Concepts | Steroid (T110) , Pharmacologic Substance (T121) |
MSH | C089740 |
SnomedCT | 699678007 |
English | 17-(3-pyridyl)androsta-5,16-dien-3beta-ol, Androsta-5,16-dien-3-ol, 17-(3-pyridinyl)-, (3beta)-, abiraterone, 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol, ABIRATERONE, Abiraterone (substance), Abiraterone |
Spanish | abiraterona, abiraterona (sustancia) |
Ontology: Androgen Synthesis Inhibitors (C3853002)
Concepts | Pharmacologic Substance (T121) |
MSH | D065088 |
English | Synthesis Inhibitors, Androgen, Inhibitors, Androgen Synthesis, Androgen Synthesis Inhibitors |