We aimed to assess the effect of a functional polymorphism of CYP3A5 on lumefantrine pharmacokinetics. Sixty-nine women diagnosed with malaria received standard doses of artemether-lumefantrine. Concentration-time data for lumefantrine and genotyping data were obtained for each participant. Pharmacokinetic-genotype associative relationships were assessed using linear regressions, Mann-Whitney U-test or Kruskal-Wallis statistics. Average age and weight (standard deviation) of the patients were 33 (6.8) years and 59.5 (11.6) kg, respectively.  genotype associated with the log-transformed maximum concentration with the median (interquartile range) values of 8279 (6516-13,420) and 6331 (4093-8631) ng/ml (p = 0.032) among the carriers and noncarriers of , respectively. Besides, the c.152-1089T>C genotypes had an associative trend with the lumefantrine area under the curve (AUC) and clearance. *3 genetic variant is associated with a high maximum plasma concentration of lumefantrine. This warrants further investigations on the association between gene variants, lumefantrine pharmacokinetics and electrophysiological effect.

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http://dx.doi.org/10.2217/pgs-2020-0081DOI Listing

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