Drug intelligence / Profile preview

everolimus + letrozole

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Everolimus (RAD001) plus letrozole is a combination therapy investigated primarily for hormone receptor-positive breast cancer. Everolimus is an orally bioavailable small molecule inhibitor of the mammalian target of rapamycin (mTOR), a key regulator of cell growth and proliferation. By inhibiting mTOR, everolimus can reduce tumor cell proliferation and angiogenesis. Letrozole is a nonsteroidal aromatase inhibitor that decreases estrogen production by blocking the conversion of androgens to estrogens, thereby slowing or stopping the growth of estrogen-dependent breast cancer cells[1][3][5]. The rationale for combining these agents is to enhance anti-tumor efficacy and potentially overcome resistance to endocrine therapy in breast cancer[3][5]. Clinical studies have shown that this combination has promising anti-tumor activity with manageable safety profiles in postmenopausal women with hormone receptor-positive breast cancer[2][5][6].**

Brand names
AfinitorFemara
Other names
RAD001 + letrozole
02

Targets

Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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