Volume 86, Issue 1
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645



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 ( = 27), mean [SD] parameters were C: 58.9 [12.5] ng/mL; t: 3.7 [1.5] h; area under concentration-time curve (AUC): 3,387 [1,328] ng/h/mL; Vλ/F: 2,829 [1,267] L; CL/F: 2.76 [1.28] L/h; and t: 784 [347] h. Compared with fasted subjects, fed subjects ( = 27) exhibited a 34% increase in C, delay in t to 5.3 [2.1] h, 44% increase in AUC, 40% decrease in Vλ/F, and a 35% decrease in CL/F. There was no significant change in t. 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.

[open-access] Freely available online through the Open Access option.


Article metrics loading...

The graphs shown below represent data from March 2017
Loading full text...

Full text loading...



  1. APOC, 2005. Final communique: eleventh session of the Joint Action Forum. Available at: http://www.who.int/apoc/about/structure/jaf/en/index.html. Accessed November 2, 2010. [Google Scholar]
  2. World Health Organization, 2010. Working to overcome the global impact of neglected tropical diseases: first WHO report on neglected tropical diseases. Available at: http://www.who.int/neglected_diseases/2010report/en/. Accessed November 8, 2010. [Google Scholar]
  3. Basáñez M-G, Boussinesq M, , 1999. Population biology of human onchocerciasis. Philos Trans R Soc Lond B Biol Sci 354: 809826.[Crossref] [Google Scholar]
  4. Plaisier AP, van Oortmarssen GJ, Remme J, Habbema JD, , 1991. The reproductive lifespan of Onchocerca volvulus in West African savanna. Acta Trop 48: 271284.[Crossref] [Google Scholar]
  5. Cotreau MM, Warren S, Ryan JL, Fleckenstein L, Vanapalli SR, Brown KR, Rock D, Chen C-Y, Schwertschlag US, , 2003. The antiparasitic moxidectin: safety, tolerability, and pharmacokinetics in humans. J Clin Pharmacol 43: 11081115.[Crossref] [Google Scholar]
  6. Forrester SG, Prichard RK, Beech RN, , 2002. A glutamate-gated chloride channel subunit from Haemonchus contortus: expression in a mammalian cell line, ligand binding, and modulation of anthelmintic binding by glutamate. Biochem Pharmacol 63: 10611068.[Crossref] [Google Scholar]
  7. Cully DF, Vassilatis DK, Liu KK, Paress PS, Van der Ploeg LH, Schaeffer JM, Arena JP, , 1994. Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans . Nature 371: 707711.[Crossref] [Google Scholar]
  8. Zulalian J, Stout SJ, daCunha AR, Garces T, Miller P, , 1994. Absorption, tissue distribution, metabolism, and excretion of moxidectin in cattle. J Agric Food Chem 42: 381387.[Crossref] [Google Scholar]
  9. Parks V, Patat A, Mayer P, Fleckenstein L, Weber W, , 2004. Relative bioavailability of liquid and tablet formulations of the antiparasitic moxidectin. Clin Exp Pharmacol Physiol 31: 128. [Google Scholar]
  10. Wu C-Y, Benet LZ, , 2005. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 22: 1123.[Crossref] [Google Scholar]
  11. Gershkovich P, Hoffman A, , 2007. Effect of a high-fat meal on absorption and disposition of lipophilic compounds: the importance of degree of association with triglyceride-rich lipoproteins. Eur J Pharm Sci 32: 2432.[Crossref] [Google Scholar]
  12. Chen YC, Hung YP, Fleckenstein L, , 2002. Liquid chromatographic assay of moxidectin in human plasma for application to pharmacokinetic studies. J Pharm Biomed Anal 29: 917926.[Crossref] [Google Scholar]

Data & Media loading...

  • Received : 28 Jun 2011
  • Accepted : 09 Sep 2011
  • Published online : 01 Jan 2012

Most Cited This Month

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error