Abiraterone (Zytiga)

General information

Class/mechanism: Antiandrogen, androgen biosynthesis inhibitor, CYP17 inhibitor. Inhibits the 17 α-hydroxylase/C17,20-lyase (CYP17) enzyme that is required for androgen biosynthesis, leading to a decrease in androgen production in testicular, adrenal, and prostate tumor tissues.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Prostate cancer

Patient drug information

• Abiraterone (Zytiga) package insert
• Abiraterone (Zytiga) patient drug information (Chemocare)
• Janssen CarePath patient support resources
• Abiraterone (Zytiga) patient drug information (UpToDate)

History of changes in FDA indication

• 2011-04-28: FDA approved to treat patients with late-stage (metastatic) castration-resistant prostate cancer who have received prior docetaxel (chemotherapy). (Based on COU-AA-301)
• 2012-12-10: FDA approved to treat men with late-stage (metastatic) castration-resistant prostate cancer prior to receiving chemotherapy. (Based on COU-AA-302)
• 2018-02-07: FDA approved in combination with prednisone for metastatic high-risk castration-sensitive prostate cancer (CSPC). (Based on LATITUDE)

History of changes in EMA indication

• 2011-09-05: Initial marketing authorization as Zytiga. Zytiga is indicated with prednisone or prednisolone for the treatment of metastatic castration resistant prostate cancer in adult men whose disease has progressed on or after a docetaxel-based chemotherapy regimen. (Based on COU-AA-301)
• 2012-12-18: Extension of Indication to include new population for Zytiga in combination with prednisone or prednisolone for the treatment of metastatic castration resistant prostate cancer in adult men who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated.
• 2017-11-15: Extension of Indication to include treatment of newly diagnosed high risk metastatic hormone sensitive prostate cancer (mHSCP) in adult men in combination with androgen deprivation therapy (ADT) for Zytiga plus prednisone or prednisolone.

History of changes in Health Canada indication

• 2011-07-27: Initial notice of compliance with prednisone for the treatment of metastatic prostate cancer (castration-resistant prostate cancer) in patients who have received prior chemotherapy containing docetaxel.
• 2013-05-28: New indication in combination with prednisone for the treatment of metastatic castration resistant prostate cancer (mCRPC) in patients who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy (ADT).
• 2018-02-13: New indication in combination with prednisone and androgen depletion therapy (ADT) for the treatment of patients with newly diagnosed high-risk metastatic prostate cancer, who may have received up to 3 months of prior ADT.

History of changes in PMDA indication

• 2014-07-04: Initial approval for the treatment of castration-resistant prostate cancer.
• 2018-02-16: New additional indication for the treatment of prostate cancer in patients with high-risk prognostic factors who have not received previous endocrine therapy.

Also known as

• Code name: CB-7630
• Generic name: abiraterone acetate
• Brand name: Abatitor, Abione, Abiracine, Abiracure, Abirakast, Abiramab, Abirapro, Abirataj, Abiratas, Arbitus, Ariteron, Birato, MyTera, Samtica, Xbira, Yonsa, Zabiteron, Zecyte, Zelgor, Zybuca, Zytiga, Zytix