Abiraterone
ZYTIGA
What it isCYP17A1 inhibitor blocking androgen synthesis everywhere, including the tumor; metastatic prostate cancer.
Why this oneIt blocks adrenal and intratumoral androgen production, which GnRH agents alone do not reach.
What limits itIt must be given with prednisone to prevent mineralocorticoid excess — hypertension, hypokalemia and edema. Take on an empty stomach; food raises exposure many-fold.
FDA-approved for
- prostate cancer (2011)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic castration-resistant prostate cancer (with prednisone 5 mg BID) | adult male | 1000 mg QD | 1000 mg QD | 1000 mg QD |
Renal No adjustment needed
Hepatic Mild (Child-Pugh A): no adjustment; moderate (Child-Pugh B): 250 mg QD; severe (Child-Pugh C): do not use.
Instructions
- Take on an empty stomach — at least 1 hour before or 2 hours after a meal.
- Swallow tablets whole with water; do not crush or chew.
- Give concurrently with a GnRH analog, or use after bilateral orchiectomy.
- Interrupt, reduce, or discontinue for hepatotoxicity per LFT monitoring.
- Should not be handled by females who are or may become pregnant.
Cautions
- Mineralocorticoid excess — hypertension, hypokalemia, fluid retention; QT prolongation/Torsades reported with hypokalemia
- Adrenocortical insufficiency (especially with prednisone withdrawal or stress)
- Hepatotoxicity, including fulminant hepatitis and acute liver failure
- Increased fractures and mortality when combined with radium Ra-223 dichloride — not recommended
- Embryo-fetal toxicity (male fertility/contraception)
- Severe hypoglycemia when used with thiazolidinediones or repaglinide in diabetics
Adverse reactions
- Common (≥10%): fatigue, arthralgia, hypertension, nausea, edema, hypokalemia, hot flush, diarrhea, vomiting, upper respiratory infection, cough, headache
- Labs (>20%): anemia, elevated alkaline phosphatase, hypertriglyceridemia, lymphopenia, hypercholesterolemia, hyperglycemia, hypokalemia
Pregnancy Not indicated in females; can cause fetal harm and loss of pregnancy (animal data).
Lactation Not indicated in females; no information on presence in human milk.
NO BOXED WARNINGS
Principal riskMineralocorticoid excess unless prednisone is co-given
Cost, est. cash$500–$15,000/month
Generic entry2018
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.
Mechanism of action: Abiraterone ballicule
Open Abiraterone in the interactive console ↗
Memory aids: mascots and interaction avatars
Zytiger = Zebra + Tiger hybrid
Abiraterone Inhibits CYP17A1: It targets 17α-hydroxylase and C17,20-lyase enzymes
