molecules of the month


oral CETP inhibitor

Ph. III candidate in cardiology

Signif. lipid lowering effect at 5 mg PO QD

Nat. Med.

NewAmsterdam Pharma B.V., Naarden, NL (Amgen)

obicetrapib chemical structure oral CETP inhibitor - Monash University, Clayton, AU NewAmsterdam Pharma B.V., Naarden, NL
5 mins read

Context. Obicetrapib (Monash University and NewAmsterdam Pharma) is an oral selective cholesteryl ester transfer protein (CETP) inhibitor being developed for dyslipidemia. Patients with high cardiovascular risk typically aim to lower cholesterol with a combination of statins, diet, and exercise, but this is often not enough. A foundational study in 1990 observed that individuals with CETP mutations showed lower LDL cholesterol and increased levels of HDL cholesterol, leading to the development of CETP inhibitors such as torcetrapib, dalcetrapib, evacetrapib, and anacetrapib. Off-target effects or lack of efficacy stalled the development of torcetrapib, dalcetrapib, and evacetrapib while anacetrapib reduced coronary events but was associated with adipose tissue retention making anacetrapib inappropriate for frequent dosing. The next generation CETP inhibitor, obicetrapib, demonstrated greater…

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