Abiraterone Dosage

Medically reviewed by Drugs.com. Last updated on Sep 5, 2023.

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

Usual Adult Dose for:

Prostate Cancer

Additional dosage information:

Renal Dose Adjustments
Liver Dose Adjustments
Dose Adjustments
Precautions
Dialysis
Other Comments

Usual Adult Dose for Prostate Cancer

Metastatic CRPC:

Regular formulation: 1000 mg orally once daily (in combination with methylprednisolone 5 mg orally 2 times daily)
Micronized formulation: 500 mg orally once daily (in combination with methylprednisolone 4 mg orally 2 times daily)

Metastatic high-risk CSPC:

Regular formulation: 1000 mg orally once daily (in combination with methylprednisolone 5 mg orally once daily)

Comments:

Patients receiving this drug should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy.
Different abiraterone acetate formulations have different indications and different dosing. Refer to the manufacturer product information before prescribing this drug.

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

No adjustment recommended.

Liver Dose Adjustments

REGULAR FORMULATION:

Mild liver impairment (Child-Pugh A): No adjustment recommended.
Moderate liver impairment (Child-Pugh B): Reduce the starting dose to 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):

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.

MICRONIZED FORMULATION:

Mild liver impairment (Child-Pugh A): No adjustment recommended.
Moderate liver impairment (Child-Pugh B): Reduce starting dose to 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 impairment (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) in patients with baseline moderate hepatic impairment:

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.

Dose Adjustments

REGULAR FORMULATION:
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 coadministration 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 coadministration period.

MICRONIZED FORMULATION:
CONCOMITANT USE OF STRONG CYP450 3A4 INDUCER:

Avoid concomitant use if possible.
If concomitant use is necessary, increase the dosing frequency to 5000 mg orally 2 times a day during the coadministration 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 coadministration period.

Precautions

CONTRAINDICATIONS:

None

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

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration Advice:

NOTE: Different products are not interchangeable.
This drug should be taken on an empty stomach at least one hour before or at least two hours after a meal with the exception of the micronized formulation which may be taken with or without food.
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)