Drug intelligence / Profile preview

everolimus + letrozole + leuprolide

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

Overview

A combination therapy consisting of three pharmaceutical agents: - Everolimus is an oral mTOR inhibitor that blocks the mammalian target of rapamycin pathway, thereby inhibiting cell growth and proliferation. - Letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme. - Leuprolide is a gonadotropin-releasing hormone receptor agonist that initially stimulates and then downregulates pituitary gonadotropin secretion, leading to suppression of sex steroid production. This combination has been studied primarily in hormone receptor-positive, HER2-negative metastatic breast cancer in premenopausal women with ovarian suppression[1], as well as in advanced fibrolamellar carcinoma[2][3]. The rationale for combining these agents is to achieve profound estrogen deprivation while simultaneously blocking mTOR signaling pathways implicated in tumor growth. All three drugs are FDA-approved for various indications individually; their use together constitutes an off-label or investigational regimen.

Other names
RAD001RAD-001RAD 001EVELETLEUleuprorelin
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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