Drug intelligence / Profile preview

letrozole

Development stage
Approved
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Letrozole is a nonsteroidal aromatase inhibitor used primarily to treat hormone receptor-positive breast cancer in postmenopausal women. It works by inhibiting the enzyme aromatase, which converts androgens into estrogens in peripheral tissues. By reducing estrogen levels, letrozole slows or stops the growth of certain types of breast cancer cells that require estrogen for proliferation. Letrozole is typically administered orally as a tablet once daily and may be used as first-line therapy, following surgery or radiation, after prior treatment with tamoxifen, or for advanced/metastatic disease. Beyond its primary indication in breast cancer, letrozole has also been studied off-label for conditions such as infertility (ovulation induction), gynecomastia, endometriosis, and other hormonally sensitive tumors[1][4][5][9].

Brand names
Femara
Other names
letrozole
02

Targets

CYP19A1 (Aromatase)CYP2C19 (Cytochrome P450 2C19)CYP2A6 (Cytochrome P450 2A6)

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