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abiraterone acetate (Zytiga)

Indications: - treatment of prostate cancer* - metastatic prostate cancer [4]* - metastatic castration-resistant prostate cancer * initial FDA approval for prostate cancer that has progressed after treatment with docetaxel [4] * metastatic prostate cancer with no or mild symptoms after failed androgen deprivation therapy (NICE) Dosage: - 1000 mg QD - in combination with prednisone or prednisolone before chemotherapy (NICE) - in combination with prednisone or prednisolone & androgen deprivation therapy [6] Adverse effects: - inhibits cortisol synthesis - syndrome of secondary mineralocorticoid excess a) hypokalemia b) hypertension c) fluid overload Mechanism of action: - inhibits CYP17A1 - inhibits corticosteroid synthesis - inhibits extragonadal androgen synthesis (adrenal DHEA synthesis)

General

enzyme inhibitor antineoplastic agent (chemotherapeutic agent)

Database Correlations

PUBCHEM correlations

References

  1. Attard G et al Selective inhibition of CYP17 with abiraterone acetate is highly active in the treatment of castration-resistant prostate cancer. J Clin Oncol 2009 Aug 10; 27:3742. PMID: 19470933
  2. Reid AHM et al. Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate. J Clin Oncol 2010 Feb 16; [e-pub ahead of print] PMID: 20159823 http://dx.doi.org/10.1200/JCO.2009.24.6819
  3. de Bono JS et al Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med. 2011 May 26;364(21):1995-2005. PMID: 21612468 - Antonarakis ES and Eisenberger MA. Expanding treatment options for metastatic prostate cancer. N Engl J Med 2011 May 26; 364:2055. PMID: 21612475
  4. FDA News Release: Dec. 10, 2012 FDA expands Zytiga's use for late-stage prostate cancer http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm331492.htm
  5. Ryan CJ et al Abiraterone in Metastatic Prostate Cancer without Previous Chemotherapy N Engl J Med. December 10, 2012 PMID: 23228172 http://www.nejm.org/doi/full/10.1056/NEJMoa1209096
  6. James ND, de Bono JS, Spears MR et al Abiraterone for Prostate Cancer Not Previously Treated with Hormone Therapy. N Eng J Med. June 3, 2017 PMID: 28578639 http://www.nejm.org/doi/full/10.1056/NEJMoa1702900 - Fizazi K, Tran N, Fein L et al Abiraterone plus Prednisone in Metastatic, Castration-Sensitive Prostate Cancer. N Eng J Med. June 4, 2017 PMID: 28578607 http://www.nejm.org/doi/full/10.1056/NEJMoa1704174
  7. Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019