Table 2.

DSM265 activity against P. falciparum parasites at different stages in the life cycle.

Assay	MPC or EC50 (μg/mL)	Fraction unbound in assay media	a Unbound MPC or EC50 (μg/mL)
Blood-stage: P. falciparum 3D7 in vitro MPC (kill assay)	0.014 a	0.17 b	0.0020
SCID mouse in vivo MPC (plasma)	1.1c	0.001d	0.0011
Blood-stage: P. falciparum 3D7 in vitro growth assay	0.0046 a	0.17b	0.00078
Liver-stage: P. falciparum – schizont	0.0057	0.215e	0.0012
P. falciparum early stage gametocytes stage III – IV; strain NF54	> 0.42	0.004f	>0.0017
Gametocyte assay P. falciparum stages IV–V	Inactive > 16	ND	ND
P. falciparum dual gamete formation assay	Inactive > 42	ND	ND
P. falciparum stage V oocyst	38% at 1.0	0.001d	38% at 0.001

Data represent EC₅₀ values unless otherwise stated to be the MPC.

^adata taken from Fig. 2D;

^b0.5% Albumax II in RPMI-1640;

^cblood to plasma ratio in the humanized SCID mouse of 0.5 was used to convert blood concentrations to plasma concentrations;

^dhuman plasma;

^e10% fetal calf serum in DMEM or similar medium;

^f10% human serum in RPMI 1640.

ND=not determined. See Table S9 for protein binding data in serum and various media.