Drug intelligence / Profile preview

alpelisib + metformin

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

Overview

Alpelisib + metformin is a combination of two small molecule drugs used together, primarily in the context of managing advanced or metastatic breast cancer with PIK3CA mutations. Alpelisib is an oral phosphatidylinositol-3-kinase alpha (PI3Kα) inhibitor that targets the PI3K pathway, which is frequently mutated in certain cancers and drives tumor growth. Its main approved indication is for use with fulvestrant in hormone receptor-positive, HER2-negative advanced breast cancer. A common and significant side effect of alpelisib therapy is hyperglycemia due to its on-target inhibition of PI3Kα signaling in insulin-responsive tissues. Metformin, a first-line oral antihyperglycemic agent and insulin sensitizer commonly used for type 2 diabetes mellitus, is co-administered to prevent or manage alpelisib-induced hyperglycemia. The combination does not represent a fixed-dose pharmaceutical product but rather a clinical management strategy where both drugs are prescribed concurrently to optimize cancer treatment efficacy while minimizing metabolic complications[1][2][4].

02

Targets

ND1 (Mitochondrial electron transport chain complex I)AMPK (Adenosine monophosphate–activated protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)

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