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- Title
Pharmacokinetic, Pharmacodynamic, and Safety Profile of a New Cholesteryl Ester Transfer Protein Inhibitor in Healthy Human Subjects.
- Authors
Wolk, R.; Chen, D.; Clark, R. W.; Mancuso, J.; Barclay, P. L.
- Abstract
A new cholesteryl ester (CE) transfer protein (CETP) inhibitor (CP-800,569) was evaluated. Doses of 30–1,800 mg were administered once daily to healthy subjects for 14 days. Serum CP-800,569 levels increased, and CETP activity decreased, in a dose-related manner. Serum levels of high-density lipoprotein (HDL) increased (by a maximum of 156%), and those of low-density lipoprotein (LDL) decreased (by a maximum of 47%). CP-800,569 also had the effect of lowering postprandial triglyceride levels. Trough concentrations of apolipoprotein E (apoE) increased: the maximum increases were 89% for total plasma apoE and 280% for HDL apoE. By contrast, the postprandial increases in total plasma levels of apoE and non HDL apoE were either diminished by CP-800,569 or reversed to decreases. CP-800,569 was very well tolerated, with some nonserious gastrointestinal adverse events seen only with the 1,800-mg dose. No changes in blood pressure (BP) were observed. The possible effects of higher CP-800,569 doses on aldosterone and cortisol levels could not be excluded. The results of this study may be useful in CP-800,569 dose selection.
- Subjects
PHARMACOKINETICS; PHARMACODYNAMICS; LIPOPROTEINS; TRIGLYCERIDES; ALDOSTERONE; BLOOD pressure
- Publication
Clinical Pharmacology & Therapeutics, 2009, Vol 86, Issue 4, p430
- ISSN
0009-9236
- Publication type
Article
- DOI
10.1038/clpt.2009.120