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exemestane (Aromasin)

Indications: 1) treatment of advanced breast cancer in postmenopausal women with disease progression despite tamoxifen therapy [3] 2) 5 year disease-free survival in premenopausal women higher with exemestane than with tamoxifen (91.1% vs. 87.3%) [6] 3) prophylaxis for breast cancer in high-risk women [4] - post-menopausal women with atypical ductal hyperplasia [4] Dosage: Storage: - store in orginal container Adverse effects: - osteoporosis: increased bone loss [5] - vasomotor symptoms - arthragia - headaches - insomnia [8] Clinical significance: Clinical trial: - 4742 women who had received 2-3 years of tamoxifen tamoxifen vs exemestane for an additional 2-3 years - disease-free survival 87% (tamoxifen) vs 92% (exemestane) - thromboembolic events less in exemestane group - new cancers (non breast cancer) fewer in exemestane group - no difference in mortality [2]

Interactions

drug adverse effects of aromatase inhibitors

General

antineoplastic endocrine agent aromatase inhibitor

Properties

INHIBITS: cytochrome P450 19A1

Database Correlations

PUBCHEM cid=60198

References

  1. Kaiser Permanente Northern California Pharmacy update, 11/2000
  2. Journal Watch 24(7):58, 2004 Coombes RC et al, N Engl J Med 350:1081, 2004 PMID: 15014181 Piccart-Gebbart MJ, N Engl J Med 350:1040, 2004
  3. New Evidence Supports the Third-generation Aromatase Inhibitor Exemestane (Aromasin) for Primary Breast Cancer Prescriber's Letter 11(4):22 2004 Detail-Document#: 200408 (subscription needed) http://www.prescribersletter.com
  4. Goss PE et al Exemestane for Breast-Cancer Prevention in Postmenopausal Women N Eng J Med June 4, 2011 PMID: 21639806 http://www.nejm.org/doi/full/10.1056/NEJMoa1103507#t=articleTop
  5. Cheung AM et al Bone density and structure in healthy postmenopausal women treated with exemestane for the primary prevention of breast cancer: a nested substudy of the MAP.3 randomised controlled trial. Lancet Oncol. 2012 Feb 6. PMID: 22318095 http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(11)70389-8/abstract - Cauley JA Bone loss associated with prevention of breast cancer Lancet Oncol. 2012 Feb 6. PMID: 22318094 http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045%2812%2970030-X/fulltext
  6. Pagani O et al Adjuvant Exemestane with Ovarian Suppression in Premenopausal Breast Cancer. N Engl J Med. June 1, 2014 PMID: 24881463 http://www.nejm.org/doi/full/10.1056/NEJMoa1404037
  7. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  8. Medical Knowledge Self Assessment Program (MKSAP) 18, American College of Physicians, Philadelphia 2018