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Oral formulations of abiraterone

Drugs List

  • abiraterone acetate 1g tablets
  • abiraterone acetate 500mg tablets
  • ZYTIGA 500mg tablets
  • Therapeutic Indications


    Metastatic castration-resistant prostate cancer
    Metastatic hormone sensitive prostate cancer

    Indicated for use with prednisone or prednisolone for the treatment of:

    Newly diagnosed high risk metastatic hormone sensitive prostate cancer in combination with androgen deprivation therapy.

    Metastatic castration-resistant prostate cancer where the disease has progressed on or after a docetaxel-based chemotherapy regimen.

    Metastatic castration-resistant prostate cancer patients who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy where chemotherapy is not yet indicated.


    Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.


    Metastatic hormone sensitive prostate cancer: 1g once daily, taken with 5mg dose prednisone or prednisolone.

    Metastatic castration-resistant prostate cancer: 1g once daily, taken with 10mg dose prednisone or prednisolone.

    Additional Dosage Information

    ALT or AST greater than 5 times ULN:
    Interrupt treatment until liver function tests have returned to baseline; re-administer abiraterone acetate at a reduced dose of 500mg once daily.

    If hepatotoxicity reoccurs at this reduced dose, treatment should be discontinued.

    ALT or AST greater than 20 times ULN:
    Discontinue treatment.

    Grade 3 or greater toxicities
    Suspend treatment and initiate appropriate medical management. Re-initiate once symptoms resolve to grade 1 or baseline.


    Long QT syndrome
    Severe hepatic impairment
    Torsade de pointes
    Uncontrolled hypertension

    Precautions and Warnings

    Family history of long QT syndrome
    Fluid retention
    Restricted sodium intake
    Cardiac failure
    Diabetes mellitus
    Electrolyte imbalance
    Glucose-galactose malabsorption syndrome
    Hepatitis B
    Hepatitis C
    History of cardiovascular disorder
    History of torsade de pointes
    Lactose intolerance
    Moderate hepatic impairment
    Recent myocardial infarction
    Severe angina
    Severe renal impairment
    Unstable angina
    Ventricular arrhythmias

    Consider supplementary corticosteroids if subject to stress or surgery
    Contains more than 1 mmol (23 mg) sodium per dose
    Control cardiac failure before starting treatment
    Correct electrolyte disorders before treatment
    Ensure hypertension is controlled prior to treatment
    Treat concurrently with a corticosteroid
    Treatment to be prescribed under the supervision of a specialist
    Contains lactose
    Advise patient to have no food for 2 hours before and 1 hour after dose
    Consult local policy on the safe use of oral anti-cancer drugs
    Staff: Not to be handled by pregnant staff
    Correct hypokalaemia before treatment
    Monitor serum transaminases before treatment
    CCF risk: Monitor BP, serum K+ & fluid retention every 2 weeks for 3months
    If hypokalaemia occurs, maintain serum potassium at or above 4 mmol/l
    Monitor blood glucose closely in patients with diabetes mellitus
    Monitor blood pressure, serum potassium and fluid retention monthly
    Monitor ECG in patients at risk of QT prolongation
    Monitor serum electrolytes
    Monitor serum transaminases every 2 weeks for 3 months, then monthly
    Consider discontinuing therapy if significant cardiac failure develops
    May cause loss of bone mineral density
    May affect results of some laboratory tests
    Discontinue permanently if AST or ALT level exceeds 20 x ULN
    Interrupt therapy if hepatic transaminases > 5 times upper limit of normal
    Interrupt treatment for any grade 3 toxicity
    Advise patient not to take St John's wort concurrently
    Male: Additional contraception required in addition to barrier method
    Male: Use of condoms advised if partner pregnant or may become pregnant

    Patients previously treated with ketoconazole for prostate cancer may have a lower rate of response to abiraterone acetate.

    Medical castration with LHRH analogue should be continued during treatment in patients not surgically castrated.

    Before starting treatment, patients with a significant risk of congestive cardiac failure should be considered for an assessment of cardiac function (e.g. echocardiogram). Cardiac failure should be treated and cardiac function optimized. During treatment, blood pressure, serum potassium and fluid retention should be monitored every 2 weeks for the first 3 months and monthly thereafter.

    Cases of myopathy and rhabdomyolysis have been reported within the first 6 months of treatment, and recovered after withdrawing treatment.

    Cases of QT prolongation have been observed in patients experiencing hypokalaemia associated with abiraterone acetate.

    Pregnancy and Lactation


    Abiraterone is not indicated for use in women.


    Abiraterone is not indicated for use in women.


    Advise patient if a dose of either abiraterone acetate, prednisone or prednisolone is missed, treatment should be resumed the following day with the usual daily dose.

    Advise patient a condom is required if engaging in sexual activity with a pregnant woman. If engaging in sexual activity with a women of child bearing potential then a condom and another effective method of contraception is required.

    Side Effects

    Acute hepatic failure
    Adrenal cortex insufficiency
    Allergic alveolitis
    Anaphylactic reaction
    Angina pectoris
    Atrial fibrillation
    Cardiac failure
    Congestive cardiac failure
    Decreased ejection fraction
    Fulminant hepatitis
    Increase in ALT level
    Increase in AST level
    Myocardial infarction
    Peripheral oedema
    Prolongation of QT interval
    Serum bilirubin increased
    Urinary tract infections
    Ventricular dysfunction

    Effects on Laboratory Tests

    Spironolactone binds to the androgen receptor and may increase prostate specific antigen (PSA) levels.


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: September 2022

    Reference Sources

    Summary of Product Characteristics: Zytiga 500 mg film coated tablets. Janssen-Cilag Ltd. Revised December 2020.
    Summary of Product Characteristics: Abiraterone 1000mg film-coated tablets. Sandoz Limited. Revised June 2021.

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    Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content

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    FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.