Pharmacokinetics and Pharmacodynamics of Anacetrapib in Black and White Healthy Subjects

Rajesh Krishna, Ferdous Gheyas, Christy Corr, Josee Cote, Yang Liu, John Wagner, David E. Gutstein

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Anacetrapib is a cholesteryl ester transfer protein inhibitor intended for the treatment of dyslipidemia. A phase 1 study was conducted to examine the pharmacokinetics and pharmacodynamics of multiple doses of anacetrapib in black compared to white healthy subjects. Although there was no apparent race-related pharmacokinetic effect, attenuation of the lipid response was observed in black subjects. Specifically, high-density lipoprotein cholesterol percentage increased 18.1% (absolute percentage points) less in black subjects (89.9%) when compared to increases in white subjects (108.0%). Similarly, the decrease in low-density lipoprotein cholesterol was 17.8% (absolute percentage points) less in blacks (–21.2%) relative to whites (–39.0%). In contrast, there were no apparent race-related differences in cholesteryl ester transfer protein mass or activity. Anacetrapib was generally well tolerated in this study. The results of this study suggest that there may be race-related differences in pharmacodynamics of anacetrapib independent of pharmacokinetics.

Original languageEnglish
Pages (from-to)1578-1585
Number of pages8
JournalJournal of Clinical Pharmacology
Volume58
Issue number12
DOIs
StatePublished - Dec 2018
Externally publishedYes

Keywords

  • anacetrapib
  • pharmacodynamics
  • pharmacokinetics
  • race

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