Dosing &
Monitoring

How to Take ZYTIGA®(abiraterone acetate)

ZYTIGA® 1,000 mg
(four 250 mg tablets OR
two 500 mg film-coated tablets)
administered orally once daily

+ 

PREDNISONE 5 mg

administered orally twice daily

URO duo

 

†Based on ZYTIGA® 500 mg tablets compared with ZYTIGA® 250 mg tablets at the recommended daily dose of 1,000 mg.

 

Without Food

Without food
No food should be eaten for at least 2 hours before taking ZYTIGA® and for 1 hour after. 

With Water

Swallow whole with water 
Tablets should be swallowed whole with water. Do not crush or chew tablets.

With Prednisone

With prednisone
The recommended dose of prednisone is 5 mg orally twice daily.

Patients receiving gonadotropin-releasing hormone agonists should maintain this treatment during the course of treatment with ZYTIGA® + prednisone.

Drug Interactions—Based on in vitro data, ZYTIGA® is a substrate of CYP3A4. In a drug interaction trial, co-administration of rifampin, a strong CYP3A4 inducer, decreased exposure of abiraterone by 55%. Avoid concomitant strong CYP3A4 inducers during ZYTIGA® treatment. If a strong CYP3A4 inducer must be co-administered, increase the ZYTIGA® dosing frequency only during the co-administration period [see Dosage and Administration (2.3)]. In a dedicated drug interaction trial, co-administration of ketoconazole, a strong inhibitor of CYP3A4, had no clinically meaningful effect on the pharmacokinetics of abiraterone.

ZYTIGA® is an inhibitor of the hepatic drug-metabolizing enzymes CYP2D6 and CYP2C8. Avoid co-administration with CYP2D6 substrates with a narrow therapeutic index. If alternative treatments cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate drug. In a CYP2C8 drug interaction trial in healthy subjects, the AUC of pioglitazone, a CYP2C8 substrate, was increased by 46% when administered with a single dose of ZYTIGA®. Patients should be monitored closely for signs of toxicity related to a CYP2C8 substrate with a narrow therapeutic index if used concomitantly with ZYTIGA®.

For more information on Dose Modification Guidelines in Hepatic Impairment and Hepatotoxicity and information on Dose Modification Guidelines, see the dose modifications.