desbutyl Lumefantrine is an active metabolite of the antimalarial agent lumefantrine .1,2 It is formed from lumefantrine by the cytochrome P450 (CYP) isoform CYP3A4.3 desbutyl Lumefantrine is active against chloroquine-sensitive and -resistant strains of P. falciparum (IC50s = 9 and 9.5 nM, respectively).1 It inhibits the human-ether-a-go-go (hERG) potassium channel, also known as Kv11.1, in HEK293 cells expressing the human channel (IC50 = 5.49 ?M).2
1.Wong, R.P.M., Salman, S., Ilett, K.F., et al.Desbutyl-lumefantrine is a metabolite of lumefantrine with potent in vitro antimalarial activity that may influence artemether-lumefantrine treatment outcomeAntimicrob. Agents Chemother.55(3)1194-1198(2011) 2.Traebert, M., Dumotier, B., Meister, L., et al.Inhibition of hERG K+ currents by antimalarial drugs in stably transfected HEK293 cellsEur. J. Pharmacol.484(1)41-48(2004) 3.Abdullahi, S.T., Soyinka, J.O., Olagunju, A., et al.CYP2B6*6 genotype specific differences in artemether-lumefantrine disposition in healthy volunteersJ. Clin. Pharmacol.60(3)351-360(2020)