The Effect of a High-Fat Breakfast on the Pharmacokinetics of Moxidectin in Healthy Male Subjects: A Randomized Phase I Trial

• Published in: The American journal of tropical medicine and hygiene Vol. 86; no. 1; pp. 122 - 125
• Main Authors: Korth-Bradley, Joan M., Parks, Virginia, Chalon, Stephan, Gourley, Ian, Matschke, Kyle, Cailleux, Karine, Fitoussi, Serge, Fleckenstein, Lawrence
• Format: Journal Article
• Language: English
• Published: Deerfield, IL American Society of Tropical Medecine and Hygiene 01.01.2012; The American Society of Tropical Medicine and Hygiene
• Subjects: Administration, Oral; Adult; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antinematodal Agents - administration & dosage; Antinematodal Agents - pharmacokinetics; Antiparasitic agents; Area Under Curve; Biological and medical sciences; Biological Availability; Dietary Fats - administration & dosage; Dietary Fats - pharmacology; Fasting; Food-Drug Interactions; Humans; Infectious diseases; Macrolides - administration & dosage; Macrolides - pharmacokinetics; Male; Medical sciences; Middle Aged; Pharmacology. Drug treatments; Young Adult; Human; Healthy subject; Phase I trial; Fat; Parasiticide; Male; Tropical medicine; Moxidectin; Pharmacokinetics
• ISSN: 0002-9637; 1476-1645; 1476-1645
• DOI: 10.4269/ajtmh.2012.11-0415

The objective of this study was to assess the effect of a high-fat meal on the pharmacokinetics of moxidectin. Healthy male subjects were randomized to receive single oral 8 mg doses of moxidectin after an overnight fast or high-fat breakfast. In fasted subjects ( N = 27), mean [SD] parameters were C max : 58.9 [12.5] ng/mL; t max : 3.7 [1.5] h; area under concentration-time curve (AUC): 3,387 [1,328] ng/h/mL; Vλ z /F: 2,829 [1,267] L; CL/F: 2.76 [1.28] L/h; and t ½ : 784 [347] h. Compared with fasted subjects, fed subjects ( N = 27) exhibited a 34% increase in C max , delay in t max to 5.3 [2.1] h, 44% increase in AUC, 40% decrease in Vλ z /F, and a 35% decrease in CL/F. There was no significant change in t ½ . The changes are consistent with an increase in moxidectin bioavailability following administration with food. There were no clinically relevant changes in vital signs, laboratory tests, or electrocardiograms.