Pharmacokinetics and Pharmacodynamics of Anacetrapib in Black and White Healthy Subjects

Journal of Clinical Pharmacology
Rajesh KrishnaDavid E Gutstein

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.

References

Oct 16, 2003·Current Cardiology Reports·Karol E Watson
May 12, 2010·Journal of Lipid Research·Mollie RanallettaTimothy S Fisher
Oct 28, 2011·Biopharmaceutics & Drug Disposition·Rajesh KrishnaS Aubrey Stoch
Jan 17, 2012·British Journal of Clinical Pharmacology·Rajesh KrishnaS Aubrey Stoch
May 2, 2014·Journal of Clinical Pharmacology·Brett LauringJohn A Wagner
Apr 6, 2017·Clinical Pharmacology and Therapeutics·R KrishnaD E Gutstein
Aug 30, 2017·The New England Journal of Medicine·UNKNOWN HPS3/TIMI55–REVEAL Collaborative GroupMartin J Landray

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