Drug intelligence / Profile preview

fulvestrant + gedatolisib

Development stage
Unknown
Lead developer
Celcuity
Modality
Small Molecules
Administration
Intramuscular, Intravenous
01

Overview

Fulvestrant + gedatolisib is an investigational combination therapy for advanced or metastatic hormone receptor-positive, HER2-negative (HR+/HER2-) breast cancer. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates the degradation of the estrogen receptor, thereby inhibiting estrogen signaling in breast cancer cells. Gedatolisib is a potent, reversible dual inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), targeting all class I PI3K isoforms and both mTORC1 and mTORC2 complexes. This combination aims to overcome resistance mechanisms following progression on CDK4/6 inhibitors and aromatase inhibitors by simultaneously blocking hormonal signaling and key growth/survival pathways in tumor cells. The regimen is being evaluated in phase 3 clinical trials for patients with HR+/HER2- advanced breast cancer who have progressed after prior standard therapies[1][2][7].

02

Targets

mTOR (Mammalian target of rapamycin kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)ESR1 (ERα)

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