Letrozole

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Adverse-effects 6 Mechanism-of-action 7 More General Terms 8 Additional Terms 9 Internet Database 10 References

Introduction

• Tradename: Femara.

Indications

• 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]

Dosage

• 2.5 mg QD [4]

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)

• iliac artery stenosis
• intermittent claudication
• aortic dilatation
• hypertensive angiopathy

• * consider concurrent Ca+2, vitamin D & bisphosphonate treatment
  

• drug adverse effects of aromatase inhibitors

Mechanism-of-action

• inhibits biosynthesis of estradiol by inhibition of aromatase

More General Terms

• aromatase inhibitor
• antineoplastic agent (chemotherapeutic agent)

Additional Terms

• cytochrome P450 19A1 (aromatase, estrogen synthetase, CYP19A1)

Internet Database

PubChem: 3902

References

1. Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
2. Prescriber's Letter 8(2):10 2001
3. Prescriber's Letter 10(11):64 2003
4. Journal Watch 23(22):173, 2003 Goss PE et al, N Engl J Med 349:1793, 2003 [1] PMID: [2] Bryant J & Wolmark N, N Engl J Med 349:1855, 2003 Burnstein HJ, N Engl J Med 349:1857, 2003
5. 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: [3]

letrozole (Femara)