Drug intelligence / Profile preview

ezetimibe + pitavastatin (Orient Pharma Co., Ltd.)

Development stage
Unknown
Lead developer
Orient Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Tonvasca is an oral fixed-dose combination of the HMG-CoA reductase inhibitor (statin) pitavastatin and the cholesterol absorption inhibitor ezetimibe. Developed by Orient Pharma, Tonvasca is approved for the treatment of primary hypercholesterolemia and mixed dyslipidemia. Pitavastatin works by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis, which leads to an increase in LDL receptor expression and enhanced clearance of LDL-C from the blood. Ezetimibe targets the Niemann-Pick C1-Like 1 (NPC1L1) sterol transporter in the small intestine, selectively inhibiting the absorption of biliary and dietary cholesterol. Together, these complementary mechanisms of action provide a synergistic reduction in LDL-C levels with a favorable metabolic safety profile.

Brand names
Tonvasca
Other names
pitavastatin + ezetimibe同抑脂同抑脂膠囊
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)NPC1L1 (Niemann-pick C1-Like 1 transporter)ANPEP (Aminopeptidase N)

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