期刊
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE
卷 84, 期 6, 页码 892-900出版社
AMER SOC TROP MED & HYGIENE
DOI: 10.4269/ajtmh.2011.10-0409
关键词
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资金
- GlaxoSmithKline PLC.
- Paladin Labs
- Institute for One World Health
- GlaxoSmithKline
- Bharat Serum and Vaccine Ltd.
- Drugs for Neglected Diseases Initiative
- National Institute of Allergy and Infectious Diseases
- National Institutes of Health
- World Health Organization
- European Commission
- World Health Organization, Medecins Sans Frontieres (Barcelona)
This randomized, open-label study of patients in India with visceral leishmaniasis (VL) investigated the effect of food on sitamaquine and desethyl-sitamaquine pharmacokinctics. Patients were randomized to receive oral sitamaquine, 2 mg/kg/day, once a day for 21 days across four cohorts (n = 41) (fasted/fed, fed/fasted, fed/fed, and fasted/fasted) over two periods (days 1-10 and 111-21), or intravenous amphotericin B (AmB), 1 mg/kg every other day for 30 days (n = 20). Mean day 21 pharmacokinetics across the four cohorts were sitamaquine, area under curve (AUC)((0-tau)) = 6,627-8,903 ng.hr/mL, ALC((0-16)) = 4,859-6,633 ng.hr/mL, maximum plasma concentration (C(max)) = 401-570 ng/mL, apparent terminal half-life (t(1/2)) = 18.3-22.8 hr, time to reach C(max) (t(max)) = 3.5-6 hr; and desethyl-sitamaquine, ALJC((o-tau)) = 2,307-3,163 ng.hr/ mL, C(max) = 109-154 ng/mL, t(1/2) = 23.0-27.9 hr, t(max) = 2-10 hr, with no significant food effect. On-therapy adverse events were observed for sitamaquine in 4(10%) of 41 patients and for AmB in 17(85%) of 20 patients. The final clinical cure (day 180) was 85% (95% confidence interval = 70.8-94.4%) for sitamaquine and 95% (95% confidence interval = 75.1- 99.9) for AmB. Sitamaquine can be taken regardless of food intake, was generally well tolerated, and showed potential efficacy in patients with visceral leishmaniasis.
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