Drug intelligence / Profile preview

EXP3179

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

EXP3179 is a small molecule metabolite of the angiotensin II receptor blocker (ARB) losartan. It serves as the aldehyde intermediate in the metabolic pathway that converts losartan into its potent carboxylic acid metabolite, EXP3174. While EXP3174 is primarily responsible for the antihypertensive and anti-tumor effects of losartan via the blockade of the angiotensin II type-1 (AT1) receptor, EXP3179 possesses distinct pharmacological properties, including acting as a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist and exhibiting anti-inflammatory and anti-platelet activities. In the context of oncology research, specifically for pancreatic ductal adenocarcinoma (PDAC), EXP3179 is studied to differentiate the pleiotropic effects of losartan metabolism from its primary AT1-mediated mechanism of action, helping to elucidate how losartan improves chemotherapy response and reduces tumor burden.

Other names
losartan aldehyde2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxaldehyde
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NOS3 (eNOS)AGTR1 (Angiotensin II Type-1 receptor)NOX4 (NADPH oxidase 4)PPARG (Peroxisome proliferator-activated receptor gamma)VEGFR2 (Vascular endothelial growth factor receptor 2)

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