Details

Autor(en) / Beteiligte

• Brueckner, R P
• Lasseter, K C
• Lin, E T
• Schuster, B G

Titel

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

Ist Teil von

• The American journal of tropical medicine and hygiene, 1998-05, Vol.58 (5), p.645-649

Ort / Verlag

United States

Erscheinungsjahr

1998

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.