Drug intelligence / Profile preview

losartan carboxylic acid

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

Overview

Losartan carboxylic acid is the major active carboxylic acid metabolite of losartan and a **small-molecule angiotensin II receptor blocker**. It is formed in vivo after administration of losartan and contributes substantially to the antihypertensive effect by selectively antagonizing the angiotensin II type 1 receptor, thereby reducing vasoconstriction and aldosterone-mediated effects. The compound is commonly used as an analyte in pharmacokinetic, bioequivalence, and CYP2C9 phenotyping studies, and recent 2024 publications also identified it as an inhibitor of human succinyl-CoA:glutarate-CoA transferase in biochemical screening and structural studies, suggesting a possible repurposing lead for glutaric aciduria type 1. In the provided literature it is also discussed in exploratory ACE2-binding work and in environmental metabolism studies as a major transformation product of losartan.

Other names
losartan carboxylic acidlosartan acidlosartan active metabolite
02

Targets

AGTR1 (Angiotensin II Type-1 receptor)SUGCT (Succinyl-CoA:glutarate-CoA transferase)

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