Drug intelligence / Profile preview

metformin + irinotecan

Development stage
Phase 2
Lead developer
Hospital de Amor
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Metformin + irinotecan is an investigational drug combination being evaluated for the treatment of refractory metastatic or recurrent colorectal cancer. This specific therapeutic approach was the subject of a Phase II single-arm clinical trial (MetIri) conducted at Barretos Cancer Hospital in Brazil. Metformin, a biguanide small molecule traditionally used for type 2 diabetes, is being repurposed for its ability to activate AMP-activated protein kinase (AMPK), which subsequently inhibits the mechanistic target of rapamycin (mTOR) signaling pathway and alters cancer cell metabolism. Irinotecan is a cytotoxic chemotherapy agent that functions as a DNA topoisomerase 1 inhibitor, preventing DNA religation and causing double-strand breaks. The combination therapy aims to leverage the metabolic stress induced by metformin to enhance the efficacy of irinotecan in patients who have failed standard treatments.

Other names
metformin hydrochlorideirinotecan hydrochloride
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)TOP1 (DNA Topoisomerase I)mTOR (Mammalian target of rapamycin kinase)

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