Abiraterone Acetate CAS NO 154229-18-2 Inquire about Abiraterone Acetate 

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What is Abiraterone Acetate?ABIRATERONE ACETATE

Abiraterone acetate is an inhibitor of CYP17 (17?-hydroxylase/C17, 20-lyase). It is designated chemically as (3?)-17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate.

Abiraterone acetate is a white to off-white, non-hygroscopic, crystalline powder. Its molecular formula is C26H33NO2 and it has a molecular weight of 391.55. Abiraterone acetate is a lipophilic compound with an octanol-water partition coefficient of 5.12 (Log P) and is practically insoluble in water. The pKa of the aromatic nitrogen is 5.19.

What is Abiraterone Acetate used for?

Abiraterone Acetate is used as an innovative drug that offers clinical benefit to patients with hormone refractory prostate cancer (castration-resistant prostate cancer)

Abiraterone Acetate Drug Interaction

Effects of Abiraterone on Drug Metabolizing Enzymes
Abiraterone is an inhibitor of the hepatic drug-metabolizing enzyme CYP2D6. In a CYP2D6 drug-drug interaction trial, the Cmax and AUC of dextromethorphan (CYP2D6 substrate) were increased 2.8- and 2.9-fold, respectively, when dextromethorphan was given with abiraterone acetate 1,000 mg daily and prednisone 5 mg twice daily. Avoid coadministration of abiraterone acetate with substrates of CYP2D6 with a narrow therapeutic index (e.g., thioridazine).

Drugs that Inhibit or Induce CYP3A4 Enzymes
The effects of strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole) or inducers (e.g., phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital) on the pharmacokinetics of abiraterone have not been evaluated. Avoid or use with caution, strong inhibitors and inducers of CYP3A4 during treatment.

Precautions Before Using Abiraterone Acetate
  • Abiraterone may cause hypertension, hypokalemia, and fluid retention as a consequence of increased mineralocorticoid levels resulting from CYP17 inhibition
  • Adrenocortical insufficiency was reported in patients receiving Abiraterone acetate in combination with prednisone, following interruption of daily steroids and/or with concurrent infection or stress.
  • Hepatotoxicity
  • Abiraterone acetate must be taken on an empty stomach. No food should be consumed for at least two hours before the dose is taken and for at least one hour after the dose is taken.
Abiraterone Acetate side effects

Stop using abiraterone and call your doctor at once if you have a serious side effect such as:

  • nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • swelling in your ankles or feet, feeling short of breath (even with mild exertion);
  • fast or uneven heart rate;
  • pain or burning when you urinate;
  • low potassium
What should you do if you miss a dose of Abiraterone Acetate?

Skip the missed dose and take the medicine the following day on an empty stomach

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.