Drug intelligence / Profile preview

AZD0780 + ezetimibe + rosuvastatin

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZD0780 + ezetimibe + rosuvastatin is a hypothetical or investigational oral combination therapy consisting of AZD0780, ezetimibe, and rosuvastatin, designed for the treatment of hypercholesterolemia and to lower low-density lipoprotein cholesterol (LDL-C) in patients at risk for atherosclerotic cardiovascular disease (ASCVD). - **AZD0780** is a novel, oral, small-molecule proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor developed by AstraZeneca, which reduces circulating LDL-C by increasing LDL receptor recycling and hepatic uptake of LDL. It is currently in phase 3 trials as monotherapy adjunct to maximally tolerated statins[1][3][4][5]. - **Ezetimibe** is a cholesterol absorption inhibitor that blocks the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, lowering cholesterol absorption and downstream plasma LDL-C. - **Rosuvastatin** is an HMG-CoA reductase inhibitor (statin) which reduces cholesterol synthesis in the liver, upregulating LDL receptor expression and lowering LDL-C. This combination would target three complementary pathways in cholesterol metabolism for potent LDL-C lowering and cardiovascular risk reduction. There is no specific evidence that a fixed-dose combination product containing all three agents has entered clinical trials or is approved, but all drugs are individually or in dual combinations studied for cardiovascular risk.

02

Targets

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

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