Drug intelligence / Profile preview

temozolomide + metformin

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

A combination therapy consisting of temozolomide (TMZ), an alkylating agent that damages DNA in cancer cells, and metformin (MET), an anti-diabetic medication. This combination has shown synergistic effects in treating glioblastoma multiforme (GBM) by inhibiting proliferation and inducing apoptosis in both glioma cells and glioma stem cells. The combination works through multiple mechanisms including inhibition of AKT-mTOR signaling pathway, activation of AMP-activated protein kinase (AMPK), and down-regulation of SOX2 expression in TMZ-resistant cells. This combination is particularly valuable because it may overcome TMZ resistance, which is common in GBM patients.

Other names
metformin hydrochloride + temozolomide1,1-dimethylbiguanide hydrochloride + temozolomide
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)DNAND1 (Mitochondrial electron transport chain complex I)SOX2 (SRY-box transcription factor 2)

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