letrozole (Femara)
Jump to navigation
Jump to search
Introduction
Tradename: Femara.
Indications
- treatment of breast cancer in postmenopausal women
- treatment of advanced breast cancer in postmenopausal women with disease progression following antiestrogen (tamoxifen) therapy
- prophylaxis of recurrent breast cancer in patients having completed 5 years of tamoxifen therapy[4]
- in general aromatase inhibitors 1st line therapy in postmenopausal women
- ovarian cancer[6]
- promoting ovulation & facilitating pregnancy in women with polycystic ovary syndrome[7]
Dosage
Pharmacokinetics
- dimimishes estrogen levels by 95% in postmenopausal women
Adverse effects
- osteoporosis*
- hot flashes
- arthralgia
- myalgia
- sexual dysfunction
- dyslipidemia (low-grade)
- adverse cardiovascular events (generally not severe)
* consider concurrent Ca+2, vitamin D & bisphosphonate treatment
Mechanism of action
- inhibits biosynthesis of estradiol by inhibition of aromatase
More general terms
Additional terms
Component of
References
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
- ↑ Prescriber's Letter 8(2):10 2001
- ↑ Prescriber's Letter 10(11):64 2003
- ↑ 4.0 4.1 4.2 Journal Watch 23(22):173, 2003 Goss PE et al, N Engl J Med 349:1793, 2003 http://content.nejm.org/cgi/reprint/NEJMoa032312v1.pdf PMID: https://www.ncbi.nlm.nih.gov/pubmed/14551341 Bryant J & Wolmark N, N Engl J Med 349:1855, 2003 Burnstein HJ, N Engl J Med 349:1857, 2003
- ↑ Coates AS, Keshaviah A, Thurlimann B, Mouridsen H, Mauriac L, Forbes JF, Paridaens R, Castiglione-Gertsch M, Gelber RD, Colleoni M, Lang I, Del Mastro L, Smith I, Chirgwin J, Nogaret JM, Pienkowski T, Wardley A, Jakobsen EH, Price KN, Goldhirsch A. Five years of letrozole compared with tamoxifen as initial adjuvant therapy for postmenopausal women with endocrine- responsive early breast cancer: update of study BIG 1-98. J Clin Oncol. 2007 Feb 10;25(5):486-92. Epub 2007 Jan 2. PMID: https://www.ncbi.nlm.nih.gov/pubmed/17200148
- ↑ 6.0 6.1 Deprecated Reference
- ↑ 7.0 7.1 Legro RS et al Letrozole versus Clomiphene for Infertility in the Polycystic Ovary Syndrome. N Engl J Med 2014; 371:119-129. July 10, 2014 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/25006718 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1313517
- ↑ 8.0 8.1 Colleoni M, Luo W, Karlsson P et al Extended adjuvant intermittent letrozole versus continuous letrozole in postmenopausal women with breast cancer (SOLE): a multicentre, open-label, randomised, phase 3 trial. The Lancet Oncology. Nov 17, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29158011 <Internet> http://thelancet.com/journals/lanonc/article/PIIS1470-2045(17)30715-5/fulltext
Chlebowski RT, Pan K. Complexity of intermittent letrozole adjuvant therapy. The Lancet Oncology. Nov 17, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29158010 <Internet> http://thelancet.com/journals/lanonc/article/PIIS1470-2045(17)30854-9/fulltext