Drug intelligence / Profile preview

glutipyran

Development stage
Preclinical
Lead developer
RIKEN
Modality
Small Molecules
01

Overview

Glutipyran is a **small-molecule inhibitor** of glucose transporters (GLUTs), acting as a **broad-spectrum pan-GLUT inhibitor** that blocks glucose uptake in cells. It inhibits glycolytic activity and cell growth in various cancer cells, including human pancreatic cancer cells. Mechanistically, it induces metabolic disruption by blocking glucose transporter-mediated uptake, leading to suppression of both glycolytic and pentose phosphate pathway metabolites, the induction of endoplasmic reticulum stress, and inhibition of tumor growth in preclinical xenograft models. Glutipyran has demonstrated synergistic antiproliferative effects when combined with mitochondrial respiration inhibitors (e.g., metformin). It was discovered by researchers at RIKEN and the Institute of Microbial Chemistry in Japan, with studies mainly focused on its potential as an anticancer research tool and not as an approved pharmaceutical drug[1][3][5][9].

Other names
(Rac)-glutipyranrel-N-(3,4-dimethoxybenzyl)-N-((R)-3-((S)-2,2-dimethyltetrahydro-2H-pyran-4-yl)-3-phenylpropyl)furan-2-carboxamide
02

Targets

GLUT1 (Glucose transporter 1)SLC2A3 (Glucose transporter type 3)SLC2A4 (Solute carrier family 2 facilitated glucose transporter member 4)

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