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Population Pharmacokinetics of Eniporide and Its Metabolite in Healthy Subjects and Patients With Acute Myocardial Infarction

From the Department of Pharmaceutics, University of Florida, Gainesville (Dr Bhattaram, Dr Nagaraja, Dr Derendorf); Department of Clinical Pharmacokinetics (Dr Kroesser, Dr Kovar); and Department of Clinical Sciences (Dr Machnig) and Clinical Pharmacology (Dr Peters), Merck KGaA, Darmstadt, Germany.

Eniporide (EMD 96 875) is a novel and selective inhibitor of the Na⁺-H⁺ exchange (NHE-1) inhibitor. The study objectives were to identify a structural model for population pharmacokinetic analysis of eniporide and its metabolite (EMD 112 843) using nonlinear mixed-effects modeling after short-term infusion (dose: 2.5-400 mg) in healthy subjects and patients undergoing myocardial reperfusion therapy. Pooled concentrations of eniporide and its metabolite from healthy subjects (n = 153; 4815 observations) and patients (n = 304; 1465 observations) were included in the pharmacokinetic analysis. Population estimates of clearance and volume of distribution of eniporide were 29.2 L/h (24.1% coefficient of variation [CV], healthy), 20.8 L/h (28.0% CV, patients) and 20.4 L (13.1% CV, healthy), 16.9 L (24.9% CV, patients), respectively. Statistical significance was achieved for the effect of age on clearance and creatinine clearance on volume of distribution of eniporide. The impact of the covariates on eniporide pharmacokinetics is minimal to warrant any dosage adjustments in patient population.

Key Words: Eniporide • pharmacokinetics • acute myocardial infarction

Address for reprints: Hartmut Derendorf, PhD, Department of Pharmaceutics, PO Box 100494, JHMHC, University of Florida, Gainesville, FL 32610.

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