Indications for ABIRATAJ

Prostate and other male cancers

In combination with prednisone for the treatment of metastatic castration-resistant prostate cancer (CRPC) and metastatic high-risk castration-sensitive prostate cancer (CSPC).

Adult:

Take on empty stomach. Swallow whole with water. 1g once daily (in combination with oral prednisone 5mg twice daily [CRPC] or 5mg once daily [CSPC]). Also give concurrent GnRH analog or patient should have had bilateral orchiectomy. Baseline moderate hepatic impairment (Child-Pugh Class B): 250mg once daily; monitor closely; discontinue if ALT/AST >5xULN or total bilirubin >3xULN. If concomitant strong CYP3A4 inducer necessary, increase abiraterone dose frequency to twice daily during co-administration period (eg, from 1g once daily to 1g twice daily); reduce back to previous dose/frequency when CYP3A4 inducer is discontinued.

Children:

Not established.

Contraindications:

Pregnancy.

Warnings/Precautions:

Risk of mineralocorticoid excess; monitor BP, serum potassium, fluid retention at least monthly. Control hypertension and correct hypokalemia before and during treatment. Heart failure, recent MI, cardiovascular disease, ventricular arrhythmias; monitor closely. Monitor for adrenocortical insufficiency. Stress (may need higher corticosteroid dose). Monitor LFTs prior to starting treatment, every 2 weeks for the first 3 months, and monthly thereafter. Baseline moderate hepatic impairment (Child-Pugh Class B): monitor LFTs prior to initiation, weekly for the first month, every 2 weeks for the next 2 months, and monthly thereafter. Interrupt and reduce dose if hepatotoxicity (ALT/AST >5xULN or total bilirubin >3xULN) occurs; see full labeling. Permanently discontinue if concurrent ALT elevation >3xULN and total bilirubin >2xULN develops without biliary obstruction or other causes of elevation. Baseline severe hepatic impairment (Child-Pugh Class C): not recommended. Males with female partners of reproductive potential must use effective contraception during therapy and for 3 weeks after last dose. Nursing mothers: not for use in women.

Pharmacological Class:

CYP17 inhibitor.

Interactions:

Antagonized by strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentin, phenobarbital); avoid (or see Adult). Potentiates CYP2D6 substrates (eg, dextromethorphan). Avoid concomitant CYP2D6 substrates with narrow therapeutic index (eg, thioridazine); if no alternatives, use caution and consider dose reduction of substrate. Concomitant CYP2C8 substrates (eg, pioglitazone): monitor closely for toxicity.

Adverse Reactions:

Fatigue, arthralgia, hypertension, nausea, edema, hypokalemia, hot flush, diarrhea, vomiting, upper respiratory infection, cough, headache, anemia, elevated LFTs, dyslipidemia, lymphopenia, hyperglycemia; hepatotoxicity (may be severe).

Note:

Pregnant women and those of childbearing potential should not handle Abirataj tablets without protection (eg, gloves). Partners must use appropriate barrier contraception.

Metabolism:

Hepatic; >99% protein bound.

Elimination:

Fecal (primarily), renal.

Generic Availability:

NO

How Supplied:

Tabs 250mg—120; 500mg—60

Indications

Abirataj is indicated in combination with prednisone for the treatment of patients with • Metastatic castration-resistant prostate cancer (CRPC) • Metastatic high-risk castration-sensitive prostate cancer (CSPC)

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Dosage

Recommended Dose For Metastatic CRPC
The recommended dose of abirataj is 1,000 mg (two 500 mg tablets or four 250 mg tablets) orally once daily with prednisone 5 mg orally twice daily.

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Side Effects

Like all medicines, this medicine can cause side effects, although not everybody gets them.. Stop taking Abiraterone Acetate Tablet and see a doctor immediately if you notice any of the following side effects.

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Drug Interactions

Drugs That Inhibit Or Induce CYP3A4 Enzymes
In a dedicated drug interaction trial, co-administration of rifampin, a strong CYP3A4 inducer, decreased exposure of abiraterone by 55%.

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Precautions

Abirataj may cause hypertension, hypokalemia, and fluid retention increased mineralocorticoid levels resulting from CYP17 inhibition.Monitor patients for hypertension, hypokalemia, and fluid retention at least once a month.

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Pharmacology

Mechanism Of Action
Abiraterone acetate (Abirataj) is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17).

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