A Phase-I pharmacokinetic, safety and food-effect study on flubentylosin, a novel analog of Tylosin-A having potent anti- < i > Wolbachia < /i > and antifilarial activity

by Negar Alami, David C. Carter, Nisha V. Kwatra, Weihan Zhao, Linda Snodgrass, Ariel R. Porcalla, Cheri E. Klein, Daniel E. Cohen, Loretta Gallenberg, Melina Neenan, Robert A. Carr, Kennan C. Marsh, Dale J. Kempf BackgroundThe parasitic filariae responsible for onchocerciasis and lymphatic filariasis are host to an endosymbiotic bacterium,Wolbachia, which is essential to the fertility and development of the parasites. We performed a Phase-I pharmacokinetic, safety and food-effect study on single and multiple ascending doses of flubentylosin (ABBV-4083), a macrolide antibacterial with activity againstWolbachia, intended to sterilize and eliminate the parasites. MethodsSeventy-eight healthy adults were exposed to flubentylosin; 36 were exposed to single ascending 40, 100, 200, 400 or 1000 mg doses; 12 received 1000 mg in the food-effect part; and 30 received multiple ascending daily doses of 100 mg for 7 days, 200 mg for 7 or 14 days, or 400 mg for 7 or 14 days. Twenty-two subjects received placebo. ResultsMaximum concentrations (Cmax) of flubentylosin were reached after 1 –2 hours, with a half-life
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research