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Table 5 Parameter values derived from in vitro experiments

From: Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development

Parameter ARS/DHA ART LF MQ PQ
IC50 measured concentration(nM) 1.39 - 13.42 9.34 17.67
Molecular weight (g/mol) 384.4 - 528.9 378.3 535.5
IC50 concentration(ng/mL) 0.53 2.64 7.1 3.53 9.46
Binding to media of in vitro experiment (0.5% Albumax) (% bound) 82.8 82.8 99.6 85 98.1
Human plasma protein binding (% bound) 93 91.7 98.7 95.6 98.6
Human whole blood to plasma ratio 1.1 0.8 0.8 1.7 0.9
Scalar (adjusted) 2.7 1.66 0.25 5.8 1.22
IC50 (adjusted) concentration (ng/mL) 1.44 4.38 1.75 20.48 11.56
γ (Slope of concentration-effect curve) 3.72 4.61 2.24 2.63 3.48
SD of γ on log-scale 0.65 0.31 0.58 0.54 0.66
  1. ARS – artesunate, ART – artemether, DHA – dihydroartemisinin, MQ – mefloquine, PQ – piperaquine, LF – lumefantrine.
  2. Geometric mean.