Drug intelligence / Profile preview

bempedoic acid + ezetimibe

Development stage
Approved
Lead developer
Esperion Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Bempedoic acid + ezetimibe is a fixed-dose oral combination medication used to lower low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia. It is indicated for use alone or in combination with other LDL-C lowering therapies and as an adjunct to dietary changes. The drug combines two mechanisms of action: - Bempedoic acid inhibits adenosine triphosphate-citrate lyase (ACL), an enzyme involved in hepatic cholesterol synthesis, thereby reducing LDL-C production. - Ezetimibe inhibits the absorption of dietary cholesterol by blocking the Niemann-Pick C1-Like 1 (NPC1L1) transporter in the small intestine. The combination is also approved to reduce the risk of myocardial infarction and coronary revascularization procedures in adults unable to take recommended statin therapy who have established cardiovascular disease or are at high risk for a cardiovascular event[1][2][3][5][8].

Brand names
NexlizetNustendi
Other names
bempedoic acid/ezetimibe
02

Targets

ACLY (ATP-citrate synthase)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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