AJTMH Transactions of the Royal Society of Tropical Medicine and Hygiene
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Am. J. Trop. Med. Hyg., 58(5), 1998, pp. 645-649
Copyright © 1998 by The American Society of Tropical Medicine and Hygiene

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American Journal of Tropical Medicine and Hygiene, Vol 58, Issue 5, 645-649
Copyright © 1998 by American Society of Tropical Medicine and Hygiene

Research Articles


First-time-in-humans safety and pharmacokinetics of WR 238605, a new antimalarial

RP Brueckner, KC Lasseter, ET Lin, and BG Schuster

WR 238605 is an 8-aminoquinoline drug currently under development for prophylaxis and treatment of malaria. Preclinical studies have demonstrated that it has greater efficacy and less toxicity compared with primaquine. In this first-time-in-human randomized, double-blind, placebo-controlled study designed to evaluate the safety, tolerance and pharmacokinetics, WR 238605 was administered to 48 men in single oral doses ranging from four to 600 mg (base). It was well tolerated, with gastrointestinal disturbances as possible side effects. Linear kinetics were demonstrated at these doses. WR 238605 has a long absorption phase and is slowly metabolized, with a tmax of 12 hr and an elimination half-life of 14 days. These safety, efficacy and pharmacokinetic properties make this drug an excellent candidate for further testing as a prophylactic, radical curative, and terminal eradication drug.


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