Name Letrozole
Classes Anticancer/Antineoplastic Agent
Diseases Breast Cancer
Cancer

Letrozole

Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. Estrogens stimulate or maintain the growth of some breast cancers. Treatment of hormonally responsive breast cancer (i.e., estrogen and/or progesterone receptor positive or receptor unknown) has included a variety of efforts to reduce estrogen levels (ovariectomy, adrenalectomy, hypophysectomy) or inhibit estrogen effects (antiestrogens and progestational agents). In some women, these interventions result in a decrease in tumor mass or a delay in tumor progression.

Letrozole is an aromatase inhibitor indicated for:

  • Adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer 
  • Extended adjuvant treatment of postmenopausal women with early breast cancer who have received prior standard adjuvant tamoxifen therapy 
  • First and second-line treatment of postmenopausal women with hormone receptor positive or unknown advanced breast cancer
  • Letrozole tablets are taken orally without regard to meals
  • Recommended dose: 2.5.mg once daily
  • Patients with cirrhosis or severe hepatic impairment: 2.5 mg every other day 

The most common adverse reactions were-

  • hot flashes
  • arthralgia 
  • flushing
  • asthenia
  • edema
  • arthralgia
  • headache
  • dizziness
  • hypercholesterolemia
  • sweating increased
  • bone pain

 

  • Decreases in bone mineral density may occur. Consider bone mineral density monitoring
  • Increases in total cholesterol may occur. Consider cholesterol monitoring. 
  • Fatigue, dizziness and somnolence may occur. Exercise caution when operating machinery 

Contraindication

Contraindicated in patients hypersensitive to letrozole.

Letrozole is contraindicated in-

  • Women of premenopausal endocrine status
  • pregnant women