Drug intelligence / Profile preview

aristolochic acid

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

**Aristolochic acid** is a mixture of structurally related nitrophenanthrene carboxylic acids, primarily aristolochic acid I (AA-I) and aristolochic acid II (AA-II), naturally occurring in Aristolochiaceae plants and some Asarum species. It is a potent nephrotoxin and carcinogen, historically used in traditional herbal medicine for conditions like arthritis, amenorrhea, weight loss, and as an immune booster. Aristolochic acid is absorbed orally and distributed systemically; its metabolism leads to DNA adduct formation, particularly in renal tissue, contributing to mutagenesis and a unique TP53 mutational signature. The primary health risks are aristolochic acid nephropathy (rapidly progressive interstitial renal fibrosis) and urothelial carcinomas, especially of the upper urinary tract and bladder. There is no approved therapeutic application, and its use is banned or heavily restricted in many countries due to safety concerns[1][2][3][4][5][7][8].

Other names
aristolochic acidsAAAA-IAA-II
02

Targets

DNAPLA2G4A (Cytosolic phospholipase A2 alpha)

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