Drug intelligence / Profile preview

ezetimibe + pitavastatin

Development stage
Phase 3
Lead developer
Kowa
Modality
Small Molecules
Administration
Oral
01

Overview

**Ezetimibe + pitavastatin** is a fixed-dose combination medication used to treat high cholesterol, including primary hypercholesterolemia, mixed dyslipidemia, and homozygous familial hypercholesterolemia, as well as to reduce plant-based sterols in homozygous sitosterolemia[2][4]. Ezetimibe inhibits cholesterol absorption in the intestine by blocking the Niemann-Pick C1-like 1 (NPC1L1) protein, while pitavastatin is a statin that inhibits HMG-CoA reductase, thereby decreasing cholesterol synthesis in the liver[2][3][4]. The combination produces greater reductions in low-density lipoprotein cholesterol (LDL-C) and total cholesterol than either agent alone, through complementary and additive action[1][3][4][5]. Clinical trials show it is effective, well-tolerated, and safe for short- to moderate-term use, with side effects similar to statin monotherapy (headache, muscle pain, back pain, diarrhea, elevated liver enzymes)[2][3][4]. It is mainly administered in adults and is contraindicated in active liver disease and hypersensitivity to its components[4]. The combination is suitable for both primary and secondary prevention of atherosclerotic cardiovascular disease and may be particularly beneficial in patients with heightened intestinal cholesterol absorption[5].

Brand names
Pitsafe-PlusPitamed-EZPitachem EZLivastat-EZEzenon-PPevastin-PlusPitezo PlusPitsafe-EZPtvsPitadek-Z
Other names
pitavastatin/ezetimibepitavastatin plus ezetimibeezetimibe/pitavastatin
02

Targets

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

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