PMID- 27206144 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20160524 LR - 20160521 IS - 2160-763X (Print) IS - 2160-763X (Linking) VI - 1 IP - 1 DP - 2012 Jan TI - Relative Bioavailability of Liquid and Tablet Formulations of the Antiparasitic Moxidectin. PG - 32-7 LID - 10.1177/2160763X11432508 [doi] AB - The antiparasitic agent moxidectin is under development for the treatment of onchocerciasis. As the first-in-human study of moxidectin used a liquid formulation but other trials used tablets, a study was performed to determine the relative bioavailability of the 2 formulations and to gain more information about the pharmacokinetics of moxidectin. Fifty-eight healthy male participants were randomized to receive open-label moxidectin (10 mg) as a tablet (n = 29) or liquid (n = 29) formulation. The mean +/- SD pharmacokinetic parameters observed following administration of the tablet were peak concentration (Cmax) 67.1 +/- 27.4 ng/mL, time to peak concentration (tmax) 3.2 +/- 1.4 hours, area under the concentration time curve (AUC) 4403 +/- 2360 ng.h/mL, apparent volume of distribution 3635 +/- 1720 L, oral clearance 2.83 +/- 1.25 L/h, and elimination half-life 1032 +/- 502 hours. The Cmax and AUC observed following administration of the liquid formulation were 28.6% and 28.8% higher, respectively, and tmax 0.9 hours shorter compared with tablets. No serious adverse events (AEs) were observed. The most commonly reported AEs were headache, infection, diarrhea, asthenia, myalgia, and dizziness during the inpatient phase and flu syndrome, headache, and infection during the 6-month outpatient phase. There was no difference in reporting of these AEs between formulations. CI - 2012 American College of Clinical Pharmacology. FAU - Korth-Bradley, Joan M AU - Korth-Bradley JM AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. FAU - Parks, Virginia AU - Parks V AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. FAU - Patat, Alain AU - Patat A AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. FAU - Matschke, Kyle AU - Matschke K AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. FAU - Mayer, Philip AU - Mayer P AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. FAU - Fleckenstein, Lawrence AU - Fleckenstein L AD - Clinical Pharmacology, Pfizer Inc, Collegeville, PA, USAPfizer Global Research and Development, Paris/La Defense, FranceClinical Pharmacology, Wyeth Research, Paris, FranceCollege of Pharmacy, University of Iowa, Iowa City, IA, USA. LA - eng PT - Journal Article PL - United States TA - Clin Pharmacol Drug Dev JT - Clinical pharmacology in drug development JID - 101572899 OTO - NOTNLM OT - antiparasitic OT - bioavailability OT - moxidectin OT - onchocerciasis OT - pharmacokinetics EDAT- 2012/01/01 00:00 MHDA- 2012/01/01 00:01 CRDT- 2016/05/21 06:00 PHST- 2016/05/21 06:00 [entrez] PHST- 2012/01/01 00:00 [pubmed] PHST- 2012/01/01 00:01 [medline] AID - 10.1177/2160763X11432508 [doi] PST - ppublish SO - Clin Pharmacol Drug Dev. 2012 Jan;1(1):32-7. doi: 10.1177/2160763X11432508.