Drug intelligence / Profile preview

lithocholic acid

Development stage
Unknown
Modality
Small Molecules
Administration
Intraperitoneal, Oral, Dietary
01

Overview

Lithocholic acid is a **secondary bile acid** formed by bacterial action in the colon, specifically through reduction of the hydroxyl group at the 7-position of chenodeoxycholic acid. It acts primarily as a **detergent to solubilize fats for absorption** in the intestine[1][2][3]. While lithocholic acid is considered **toxic to hepatocytes at high concentrations** and has been implicated as a **carcinogen** (due to its ability to induce oxidative stress, DNA damage, and promote tumorigenesis), recent studies also suggest potential beneficial effects. These include **anti-inflammatory actions** in the colon, **activation of the TGR5 receptor**, and selective cytotoxicity against various malignancies[1][2][3][4]. LCA is also an **agonist of the vitamin D receptor**, binds NAPE-PLD to influence lipid signaling, and has shown **anti-aging effects in preclinical models**[1]. It is not currently an approved pharmaceutical but is the focus of ongoing preclinical and mechanistic research.

Other names
3α-hydroxy-5β-cholan-24-oic acid
02

Targets

GPBAR1VDR (Vitamin D receptor)NAPE-PLD (N-acyl phosphatidylethanolamine-specific phospholipase D)

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