Drug intelligence / Profile preview

alpelisib + dapagliflozin + fulvestrant + metformin

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

This is a combination therapy consisting of four medications used together for the treatment of HR+, HER2-, PIK3CA mutant metastatic breast cancer. Alpelisib is a selective PI3K inhibitor that targets the p110α isoform, blocking the PI3K/AKT/mTOR pathway which is often hyperactivated in breast cancer. Dapagliflozin is an SGLT2 inhibitor that helps manage alpelisib-induced hyperglycemia, a common side effect. Fulvestrant is an estrogen receptor antagonist that blocks estrogen receptors in breast cancer cells, preventing estrogen-stimulated tumor growth. Metformin is an antidiabetic medication that, when combined with dapagliflozin, helps normalize blood glucose levels during alpelisib treatment while maintaining the antitumor efficacy of alpelisib.

02

Targets

ESR1 (ERα)SGLT2 (Sodium-glucose cotransporter protein subunit 2)AMPK (Adenosine monophosphate–activated protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)

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