Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP)

Joseph M. Ready

doi:10.1021/acs.jmedchem.1c01540

Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP)

Joseph M. Ready

Research output: Contribution to journal › Review article › peer-review

3 Scopus citations

Abstract

Inhibitors of cholesteryl ester transfer protein (CETP) elevate HDL levels human clinical trials. However, the first CETP inhibitors proved toxic in pivotal trials or showed minimal therapeutic benefit. Anacetrapib showed some clinical benefit but is high lipophilic. This Viewpoint highlights efforts to optimize anacetrapib to a best-in-class CETP inhibitor.

Original language	English (US)
Pages (from-to)	13212-13214
Number of pages	3
Journal	Journal of Medicinal Chemistry
Volume	64
Issue number	18
DOIs	https://doi.org/10.1021/acs.jmedchem.1c01540
State	Published - Sep 23 2021

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/acs.jmedchem.1c01540

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title = "Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP)",

abstract = "Inhibitors of cholesteryl ester transfer protein (CETP) elevate HDL levels human clinical trials. However, the first CETP inhibitors proved toxic in pivotal trials or showed minimal therapeutic benefit. Anacetrapib showed some clinical benefit but is high lipophilic. This Viewpoint highlights efforts to optimize anacetrapib to a best-in-class CETP inhibitor.",

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AU - Ready, Joseph M.

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AB - Inhibitors of cholesteryl ester transfer protein (CETP) elevate HDL levels human clinical trials. However, the first CETP inhibitors proved toxic in pivotal trials or showed minimal therapeutic benefit. Anacetrapib showed some clinical benefit but is high lipophilic. This Viewpoint highlights efforts to optimize anacetrapib to a best-in-class CETP inhibitor.

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Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP)

Abstract

ASJC Scopus subject areas

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