Zytiga is a type of classification belongs to antineoplastics and it contain active ingredients of Abiraterone acetate. Which is an antiandrogen medication is indicated for the treatment of prostate cancer which spread to other parts of the body.

Zytiga is also used along with prednisone, a steroid. In clinical trials Zytiga is used for prostate cancer and advanced breast cancer.


Zytiga is an inhibitor of CYP17 which is used to treats the patients with metastatic castration-resistant prostate cancer, The patient have received earlier chemotherapy with docetaxel combination with prednisone and in failure of androgen deprivation treatment.

The patient clinically not used for chemotherapy with prednisone or prednisolone will preferred treatment with metastatic CRPC in adult men.

Mechanism Of Action

A type of steroidal enzyme inhibitor CYP17A1 (17 alpha-hydroxylase/C17,20 lyase) is known as abirateron acetate which is an orally active and It interefere with CYP17A1 in a selective and invariable manner through covalent binding mechanism. An enzyme CYP17A1 which catalyzes the biosynthesis of androgen and is highly expressed in testicular, adrenal, and prostatic tumor tissue. Particularily , abiraterone prevents the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone (DHEA) by the enzyme CYP17A1 to reduce serum levels of testosterone and other androgens.


Poorly absorbed and hydrolysis by esterases. Abiraterone acetate is a salt form, is a prodrug and have higher oral bioavailability. Time to maximum serum concentration is 1.5 – 4 hours.
Food and high fat meals increases absorption.
Protein bound to alpha – 1- acid glycoprotein and albumin is >99%
Metabolism :
By hydrolyzed Abiraterone acetate is converted into active metabolite Abiraterone through esterases. metabolized in CYP3A4 and SULT2A1
Excreted through feces (88%) and urine (5%). Terminal half life is 5-14hours.

Dosage and administration

• Prescribed dose of Zytiga tablets is 1,000 mg, Xibra 250mg given 4 dose orally once in a day (OD).
• Zytiga tablets in Combination with prednisone 5 mg administered orally twice daily.
• Zytiga Tablets administrated on an empty stomach.
• No food should be consumed for at least 2 hours before and at least 1 hour after the dose of ZYTIGA Tablets is taken.
• Zytiga should be swallowed whole with water.
• Do not crush or chew the tablets.
Abiraterone has no specific antidote, If overdose occurs stop the drug and provide general supportive measures such as monitoring arrhythmias and cardiac failure and assess liver function.


Do not take other medications, i.e prescription, over-the-counter, vitamins, herbal remedies, etc be sure to inform the doctors before the treatment. Aspirin do not administering and products containing aspirin till doctor particularily allow the drug.
• In women Abiraterone acetate is not currently used. if administrating abiraterone acetate by woman, Do not get pregnant and breastfeeding not recommended during treatment
• Unknown process of abiraterone acetate is eliminated in semen, hence do not use condom and another method of birth control by men during treatment and for 1 week following the last dose of abiraterone acetate.

Drug Interaction

• Effects of Abiraterone on drug metabolizing enzymes
Abiraterone is a hepatic drug-metabolizing inhibitor CYP2D6, when substrates (dextromethorphan) of it is co administrated with Abiraterone will increases the Cmax and AUC dextromethorphan.
• Drugs that inhibits or induce CYP3A4
Abiraterone interaction with strong CYP3A4inhibitors or inducers, the pharmacokinetics of Abiraterone is not evaluated properily, so avoid or use with caution while abiterone therapy.


Category X: Abiraterone acetate is not recommended for womens, It will cause fetal harm when administered to pregnant women. During treatment if women become pregnant, immediately stop the drug and give counseling to the women.

Side Effects

Patients taking Abiraterone acetate have following side effects are common in >30% occurring
• Retention of fluid
• Triglycerides increased
• Increased liver enzyme
Less common side effects of Abiraterone 10-29% occurring:
• Joint discomfort
• Hypokalemia
• Swelling of hands/ feets
• Myalgia
• Hypophosphatemia

Missed Dose

If missed a dose take have it as soon you remember, if time for next dose reach, then leave the missed dose and follow regular schedule. Do not take two dose at a time. TAKE ADVICE FROM THE DOCTOR.


Abiraterone acetate is not used in women excretion in human milk is unknown and the drug effects in the nursing infant is unknown.


Store the medicine in tight, closed container and kept at room temperature, away from excess heat and moisture.
Keep out of reach of children’s
Store at 200C – 250C
Pregnant women should not handle without protection e.g gloves.


Patients contraindicated with peptic ulcer, severe heart disease, stroke and hypersensitivity.

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