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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.