Drug intelligence / Profile preview

lapaquistat acetate + fenofibrate

Development stage
Phase 2
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Lapaquistat acetate + fenofibrate is a combination of two lipid-lowering agents investigated for the treatment of dyslipidemia and hypercholesterolemia. Lapaquistat acetate is a squalene synthase inhibitor that reduces cholesterol biosynthesis by blocking the conversion of farnesyl pyrophosphate to squalene, thereby lowering low-density lipoprotein cholesterol (LDL-C) and other cardiovascular risk markers. Its development was terminated due to hepatic safety concerns, including elevations in liver enzymes and rare cases meeting Hy's law criteria[1][4][5]. Fenofibrate is a fibrate derivative that acts as an agonist of peroxisome proliferator activated receptor alpha (PPARα), increasing lipolysis, activating lipoprotein lipase, reducing apoprotein CIII, and enhancing the catabolism of triglyceride-rich particles. It is approved for use in primary hypercholesterolemia, mixed dyslipidemia, and severe hypertriglyceridemia[6][7][8]. The combination was studied in clinical trials for its potential additive effects on lipid parameters[3].

Brand names
LofibraLipanthylLipidilLipantil microSupralipFenocor-67Fenocor67Fenocor 67FenogalTricheckAtorva TGGolipStanlip
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)FDFT1 (Squalene synthase)

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