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everolimus (Afinitor)

Indications: - pharmaceutical agent used in drug-eluting stent - chemotherapy for advanced kidney cancer - hormone-receptor positive breast cancer - for use in combination with Aromasin (exemestane) for treatment of postmenopausal women with advanced hormone-receptor positive, HER2-negative breast cancer [3,6] - recurrent endometrial cancer, in combination with letrozole [8] - islet cell tumor [4] - tuberous sclerosis - prevention of renal graft rejection - cardiac transplantation - liver transplantation [4] Dosage: - oral agent Storage: - store in orginal container - must be protected from light & moisture [5] Adverse effects: - proteinuria [7] - anemia, leukopenia [7] - dysplipidemia [7] - new-onset diabetes mellitus [7] - mouth ulcers, infections, rash, fatigue, diarrhea, anorexia - more common in elderly [3] Laboratory: - everolimus in blood - everolimus in dried blood spot - everolimus in plasma Mechanism of action: - antiproliferative agent - reduces intimal hyperplasia - mTOR inhibitor

Interactions

drug adverse effects of immunosuppressive agents monitor with immunosuppressive agents

General

mTOR inhibitor; target of rapamycin inhibitor

Database Correlations

PUBCHEM correlations

References

  1. Stone GW, Midei M, Newman W, Sanz M, Hermiller JB et al; SPIRIT III Investigators. Comparison of an everolimus-eluting stent and a paclitaxel- eluting stent in patients with coronary artery disease: a randomized trial. JAMA. 2008 Apr 23;299(16):1903-13. PMID: 18430909 - Patel MR, Holmes DR Jr. Next-generation drug-eluting stents: a spirited step forward or more of the same. JAMA. 2008 Apr 23;299(16):1952-3. No abstract available. PMID: 18430915
  2. Prescriber's Letter 17(2): 2010 New Drugs Approved by the FDA in 2009 Detail-Document#: 260213 (subscription needed) http://www.prescribersletter.com
  3. FDA News Release: July 20, 2012 FDA approves Afinitor for advanced breast cancer http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm312965.htm
  4. Deprecated Reference
  5. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  6. Baselga J, Campone M, Piccart M et al Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer. N Engl J Med. 2012 Feb 9;366(6):520-9 PMID: 22149876
  7. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  8. Bankhead C. Recurrent Endometrial Ca Responds to mTOR Drug. Responses in half of patients with no prior chemotherapy. MedPage Today. March 25, 2018 https://www.medpagetoday.com/meetingcoverage/sgo/71982 - Slomovitz B, et al GOG 3007, a randomized phase II trial of everolimus and letrozole or hormonal therapy (medroxyprogesterone/tamoxifen) in women with advanced, persistent, or recurrent endometrial carcinoma: A GOG Foundation study. Society of Gynecologic Oncology (SGO) 2018;Abstract 1.