Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans

International Journal of Clinical Pharmacology and Therapeutics
Troy C SarichBruce P Damiano

Abstract

To assess and validate the application of a non-radioactive assay for cholesteryl ester transfer protein (CETP) activity in clinical samples. In this Phase 0 study, CETP activity was measured following addition of the CETP inhibitor JNJ-28545595 to plasma samples from normolipidemic and three subgroups of dyslipidemic subjects with differing lipid profiles. CETP activity was elevated in plasma samples from dyslipidemic subjects compared to normolipidemic subjects. Increased triglyceride levels correlated with decreased CETP inhibition. The assay was found to have good analytical precision and high throughput potential as required for clinical trial sample analysis. The results demonstrate that pharmacological inhibition of CETP is affected by the dyslipidemic nature of plasma samples. In addition, since the optimal degree of CETP inhibition for maximal cardiovascular benefit in patients is not known, this assay may be used to help define optimal dosing of CETP inhibitors.

Citations

May 10, 2013·Clinical Pharmacokinetics·Amir Hooshang Mohammadpour, Fatemeh Akhlaghi
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Gajanan K DewkarJamal Zweit
Feb 9, 2016·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·Michael LevineUNKNOWN Lipid Emulsion Workgroup
Jan 19, 2017·Cardiology in Review·Vaughn A Eyvazian, William H Frishman

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