Abiraterone; Uses, Dosage, Side Effects, Interactions

Abiraterone; Uses, Dosage, Side Effects, Interactions

Abiraterone is an antiandrogen used to treat metastatic, castration-resistant prostate cancer. Abiraterone is associated with a not uncommon rate of serum enzyme elevation during therapy but has not been clearly linked to cases of clinically apparent liver injury with jaundice.

Abiraterone is a steroidal compound with antiandrogen activity. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex; CYP17A1), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels.

Abiraterone acetate is a steroidal CYP17A1 inhibitor and by extension androgen synthesis inhibitor which is used in combination with prednisone in metastatic castration-resistant prostate cancer (previously called hormone-resistant or hormone-refractory prostate cancer) – i.e., prostate cancer not responding to androgen deprivation or treatment with androgen receptor antagonists. It is a prodrug to the active agent abiraterone.

Mechanism of action of Abiraterone

Abiraterone is an orally active inhibitor of the steroidal enzyme CYP17A1 (17 alpha-hydroxylase/C17,20 lyase). It inhibits CYP17A1 in a selective and irreversible manner via the covalent binding mechanism. CYP17A1 is an enzyme that catalyzes the biosynthesis of androgen and is highly expressed in testicular, adrenal, and prostatic tumor tissue. More specifically, abiraterone inhibits the conversion of 17-hydroxypregnenolone to dehydroepiandrosterone (DHEA) by the enzyme CYP17A1 to decrease serum levels of testosterone and other androgens.

Indications of Abiraterone

  • Prostate Cancer
  • Metastatic Castration-Resistant Prostate Cancer
  • Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.

Contra-Indications of Abiraterone

  • Hyper sense. to drug/class/common.
  • Pregnancy
  • Uncontrolled or severe HTN
  • Hypokalemia
  • ALT >3x ULN and bilirubin >2x ULN
  • Hepatic impairment, Child-Pugh Class C
  • Hepatic impairment, Child-Pugh Class B
  • Cardiovascular dz or hx
  • Heart failure
  • Recent MI
  • Arrhythmias
  • Adrenal insufficiency
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Dosage of Abiraterone

Strengths: 250 mg; 500 mg

Prostate Cancer

  • 1,000 mg orally once a day on an empty stomach (in combination with prednisone 5 mg orally 2 times a day)

Side Effects of Abiraterone

The most common

More common

Less common

Drug Interactions of Abiraterone

Abiraterone acetate may interact with following drugs, supplements & may decrease the efficacy of the drug
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Pregnancy & Lactation of Abiraterone

 FDA Pregnancy Category X

Pregnancy

Abiraterone should not be used by women. It is not known if abiraterone is found in semen. If you are engaged in sexual activity with a pregnant woman, a condom should be used. If you are engaged in sexual activity with a woman who may become pregnant, a condom and a second effective method of birth control should be used. Condoms must be used during treatment with abiraterone and for one week after treatment has ended.Due to the way that abiraterone works, it is possible that exposure to this medication during pregnancy may harm the developing baby. To prevent accidental exposure to abiraterone, women who handle these tablets should wear gloves.

Lactation 

Abiraterone should not be used by women. It is not known if abiraterone passes into breast milk. To prevent accidental exposure to abiraterone, women who handle these tablets should wear gloves. The safety and effectiveness of using this medication have not been established for children.

References

  1. https://www.echa.europa.eu/web/guest/information-on-chemicals/cl-inventory-database/-/discli/details/248856

  2. https://pubchem.ncbi.nlm.nih.gov

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