Skip to Content

Abiraterone Dosage

Medically reviewed on July 12, 2018.

Applies to the following strengths: 125 mg; 250 mg; 500 mg

Usual Adult Dose for Prostate Cancer

NOTE: Different abiraterone acetate formulations have different indications and different dosing. Below are suggested dosing guidelines. Refer to the manufacturer product information before prescribing this drug.

YONSA (R) (micronized formulation): 500 mg once daily (in combination with methylprednisolone 4 mg orally 2 times a day)
Comments:
-Yonsa (R) can be taken with or without food.
-Patients receiving Yonsa (R) should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.
-Tablets should be swallowed whole with water; do not crush or chew.
USE: In combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer

ZYTIGA (R):
-Metastatic CRPC: 1000 mg orally once a day with prednisone 5 mg orally 2 times a day
-Metastatic high-risk CSPC: 1000 mg orally once a day with prednisone 5 mg orally once a day
Comments:
-Zytiga (R) should be taken on an empty stomach, either one 1 before or 2 hours after a meal.
-Patients receiving Zytiga (R) should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.
-Tablets should be swallowed whole with water; do not crush or chew.
USES: In combination with prednisone for the treatment of patients with:
-Metastatic castration-resistant prostate cancer (CRPC)
-Metastatic high-risk castration-sensitive prostate cancer (CSPC)

Renal Dose Adjustments

YONSA (R) (micronized formulation): No adjustment recommended.
ZYTIGA (R): No adjustment recommended.

Liver Dose Adjustments

YONSA (R) (micronized formulation):
-Mild Liver Dysfunction (Child-Pugh A): No adjustment recommended.
-Moderate Liver Dysfunction (Child-Pugh B): 125 mg orally once a day; monitor ALT, AST, and bilirubin prior to the start of therapy, every week for the first month, every 2 weeks for the following 2 months of therapy and monthly thereafter. If elevations in ALT and/or AST greater than 5 x upper limit of normal (ULN) or total bilirubin greater than 3 x ULN occur in patients with baseline moderate hepatic impairment, discontinue therapy permanently.
-Severe Liver Dysfunction (Child-Pugh C): Not recommended.
DEVELOPMENT OF HEPATOTOXICITY (ALT AND/OR AST GREATER THAN 5 X ULN OR TOTAL BILIRUBIN GREATER THAN 3 X ULN) DURING THERAPY:
-Interrupt therapy, then restart at a reduced dose of 375 mg orally once a day following return of liver function tests to baseline or to ALT and AST 2.5 x ULN or less and total bilirubin 1.5 x ULN or less. For patients who resume therapy, monitor serum transaminases and bilirubin at a minimum of every 2 weeks for 3 months and monthly thereafter.
-If hepatotoxicity recurs at 375 mg/day, then restart at a reduced dose of 250 mg orally once a day following return of liver function tests to baseline or to ALT and AST 2.5 x ULN or less and total bilirubin 1.5 x ULN or less.
-Discontinue therapy if hepatotoxicity recurs at 250 mg/day.
-Permanently discontinue therapy in patients who develop a concurrent elevation of ALT greater than 3 x ULN and total bilirubin greater than 2 x ULN in the absence of biliary obstruction or other causes responsible for the concurrent elevation.

ZYTIGA (R):
-Mild Liver Dysfunction (Child-Pugh A): No adjustment recommended.
-Moderate Liver Dysfunction (Child-Pugh B): 250 mg orally once a day
-Severe Liver Dysfunction (Child-Pugh C): Not recommended.
DEVELOPMENT OF HEPATOTOXICITY (ALT AND/OR AST GREATER THAN 5 X ULN OR TOTAL BILIRUBIN GREATER THAN 3 X ULN) DURING THERAPY:
-Interrupt therapy, then restart at a reduced dose of 750 mg orally once a day following return of liver function tests to baseline or to ALT and AST 2.5 x ULN or less and total bilirubin 1.5 x ULN or less. For patients who resume therapy, monitor serum transaminases and bilirubin at a minimum of every 2 weeks for 3 months and monthly thereafter.
-If hepatotoxicity recurs at 750 mg/day, then restart at a reduced dose of 500 mg orally once a day following return of liver function tests to baseline or to ALT and AST 2.5 x ULN or less and total bilirubin 1.5 x ULN or less.
-Discontinue therapy if hepatotoxicity recurs at 500 mg/day.
-Permanently discontinue therapy in patients who develop a concurrent elevation of ALT greater than 3 x ULN and total bilirubin greater than 2 x ULN in the absence of biliary obstruction or other causes responsible for the concurrent elevation.

Dose Adjustments

YONSA (R) (micronized formulation):
CONCOMITANT USE OF STRONG CYP450 3A4 INDUCER:
-Avoid concomitant use if possible.
-If concomitant use is necessary, increase the dosing frequency to 500 mg orally 2 times a day during the co-administration period.
-Return to the previous dosing frequency once the strong CYP450 3A4 inducer is discontinued.
CONCOMITANT USE OF CYP450 3A4 INDUCERS:
-Avoid concomitant strong CYP450 3A4 inducers during Yonsa (R) therapy.
-If a strong CYP450 3A4 inducer must be co-administered, increase the Yonsa (R) dosing frequency.
CONCOMITANT USE OF CYP450 2D6 Substrates:
-Avoid co-administration of YONSA with CYP450 2D6 substrates that have a narrow therapeutic index.
-If an alternative treatment cannot be used, exercise caution and consider a dose reduction of the concomitant CYP450 2D6 substrate.

ZYTIGA (R):
CONCOMITANT USE OF STRONG CYP450 3A4 INDUCER:
-Avoid concomitant use if possible.
-If concomitant use is necessary, increase the dosing frequency to 1000 mg orally 2 times a day during the co-administration period.
-Return to the previous dosing frequency once the strong CYP450 3A4 inducer is discontinued.
CONCOMITANT USE OF CYP450 2D6 SUBSTRATES WITH NARROW THERAPEUTIC INDEX:
-Avoid concomitant use if possible.
-If concomitant use is necessary, consider a dose reduction of the CYP450 2D6 substrate during the co-administration period.

Precautions

CONTRAINDICATIONS:
-Pregnancy (can cause fetal harm and potential loss of pregnancy)

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

YONSA (R) (micronized formulation): Data not available
ZYTIGA (R): Data not available

Other Comments

Administration Advice:
-NOTE: Different products are not interchangeable.
-This drug should be swallowed whole with water.
-Drug tablets should not be crushed or chewed.
-Pregnant women should not handle this drug without protection (e.g., gloves).
-In the event of a missed dose, the missed dose should be skipped and therapy should be resumed the following day with the usual daily dose.

Monitoring:
-Cardiovascular: Cardiac function
-Endocrine: Blood pressure, serum potassium, fluid retention, signs/symptoms of adrenocortical insufficiency
-Hepatic: ALT, AST, bilirubin
-Metabolic: Blood sugar (in diabetic patients)

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Hide