TABLE 1.

The pharmacokinetic parameters of berzosertib in FVB wild-type, Bcrp1^–/–, Mdr1a/b^–/–, Mdr1a/b^–/– Bcrp1^–/– mice after administration of a single intravenous bolus dose of 20 mg/kg

Parameter	Units	Wild-type		Bcrp1 –/–		Mdr1a/b–/–		Mdr1a/b Bcrp1–/–
		Plasma	Brain	Plasma	Brain	Plasma	Brain	Plasma	Brain
t 1/2	hour	4.16	3.51	5.27	4.4	4.31	3.80	4.88	5.47
AUC0-∞	hr*ng/ml	4860 ± 121	3097 ± 78	6524 ± 487	5500 ± 434	5562 ± 756	13,167 ± 1354	5372 ± 358	92,068 ± 11,145
Vd	L/kg	22.6	—	22	—	21.7	—	20.2	—
CL	L/hr/kg	4.1	—	3.0	—	3.6	—	3.7	—
fu		0.081 ± 0.004	0.0014 ± 0.0002	0.072 ± 0.004	0.0016 ± 0.0002	0.08 ± 0.01	0.0015 ± 0.0002	0.07 ± 0.008	0.0014 ± 0.0002