Drug intelligence / Profile preview

letrozole + megestrol

Development stage
Unknown
Lead developer
University of Cambridge
Modality
Small Molecules
Administration
Oral
01

Overview

Letrozole + megestrol is an investigational combination therapy consisting of two oral small molecule drugs, letrozole and megestrol acetate, used in the treatment of hormone receptor-positive breast cancer. Letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme, thereby reducing estrogen-driven tumor growth. Megestrol acetate is a synthetic progestin (progesterone receptor agonist) that mimics progesterone activity and has been shown to modulate estrogen receptor signaling through cross-talk with the progesterone receptor. The combination aims to enhance anti-tumor efficacy by targeting both estrogen and progesterone pathways in postmenopausal women with early-stage ER-positive breast cancer. Early clinical trial results suggest this combination may be more effective at stopping tumor growth than letrozole alone and may also help reduce side effects such as hot flushes[1][2][4].

Other names
letrozole + megestrol acetate
02

Targets

CYP19A1 (Aromatase)CYP2C19 (Cytochrome P450 2C19)PR (Progesterone receptor)CYP2A7 (Cytochrome P450, family 2, subfamily A, polypeptide 7)GR (Glucocorticoid receptor)AR (Adrenergic receptors)CYP2A6 (Cytochrome P450 2A6)

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