Drug intelligence / Profile preview

lifibrol

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

Lifibrol is a synthetic small molecule lipid-lowering agent developed as a hypocholesterolemic compound for the treatment of hypercholesterolemia and related lipid disorders. It was investigated in multiple clinical trials up to phase 3 but development was discontinued before approval[2][3][4]. Lifibrol acts through a complex mechanism distinct from statins; it reduces cholesterol absorption from the intestine, moderately decreases hepatic cholesterol biosynthesis (appearing to act as a cholesterol synthesis inhibitor), and stimulates expression of low-density lipoprotein (LDL) receptors by a sterol-independent mechanism[3][4][6][7]. In clinical studies, lifibrol significantly reduced LDL cholesterol and apolipoprotein B levels, with additional effects on triglycerides and lipoprotein(a)[5]. Unlike statins, it also lowers Lp(a), an independent risk factor for atherosclerosis[3]. Lifibrol may affect bile acid metabolism and enhance sterol excretion. The drug is racemic with no defined stereochemistry in its marketed form[7].

Other names
4-[4-(4-tert-butylphenyl)-2-hydroxybutoxy]benzoic acid
02

Targets

LDLR (Low-density lipoprotein receptor)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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