Abiraterone Acetate (Zytiga) — Clinical FAQs

Question 1

What is Abiraterone Acetate FDA-approved to treat?

Accepted Answer

Abiraterone Acetate is FDA-approved for the following oncology indications: 1. Metastatic castration-resistant prostate cancer (mCRPC) in combination with prednisone — approved 2011 (post-chemotherapy, COU-AA-301 trial) and 2012 (chemotherapy-naive, COU-AA-302 trial) 2. Metastatic high-risk castration-sensitive prostate cancer (mCSPC) in combination with prednisone or methylprednisolone and ADT — approved 2018 (LATITUDE trial).

Question 2

How does Abiraterone Acetate work (mechanism of action)?

Accepted Answer

Abiraterone is a selective, irreversible inhibitor of CYP17A1 (17α-hydroxylase/C17,20-lyase), a cytochrome P450 enzyme required for androgen biosynthesis in the testes, adrenal glands, and prostatic tumor tissue. By blocking both the 17α-hydroxylase and C17,20-lyase activities of CYP17A1, abiraterone suppresses synthesis of dehydroepiandrosterone (DHEA) and androstenedione, upstream precursors of testosterone. The resulting profound androgen deprivation suppresses signaling through the androgen receptor (AR), driving apoptosis in AR-dependent prostate cancer cells. Compensatory increases in ACTH and mineralocorticoid precursors necessitate co-administration of prednisone to prevent mineralocorticoid excess syndrome.

Question 3

How is Abiraterone Acetate administered?

Accepted Answer

Abiraterone Acetate is administered Oral (PO). Zytiga (abiraterone acetate): 1000 mg PO once daily taken on an empty stomach (no food 2 hours before or 1 hour after dose); tablets must not be crushed or chewed.

Question 4

What are the most common side effects of Abiraterone Acetate?

Accepted Answer

The most commonly reported side effects of Abiraterone Acetate (≥10% incidence) include: Hypertension (37%), Hypokalemia (28-35%), Peripheral edema (28%), Fatigue (39%), Nausea (22%) and others (10 total). Consult your oncologist for complete prescribing information.

Question 5

Is Abiraterone Acetate safe during pregnancy?

Accepted Answer

Abiraterone Acetate pregnancy safety: Pregnancy Category X (Zytiga) / Contraindicated in pregnancy. Abiraterone causes fetal harm and is contraindicated in women who are or may become pregnant. Males with female partners of reproductive potential should use effective contraception during and for 3 weeks after last dose.. Oncologists should review the complete prescribing information and discuss reproductive risks with patients before initiating therapy.

Abiraterone Acetate — Drug Monograph

Mechanism of Action

FDA Indications

Common Side Effects

Clinical Pearl

Related Therapies & Mechanisms