Table 1 The preclinical pharmacokinetics of EZM2302 determined in mouse and rat.

From: Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma

Parameter

CD-1 mouse

Sprague-Dawley rat

IV Bolus

PO

IV Bolus

PO

Dose (mg/kg)

2

10

2

10

Blood:plasma ratio

1.2

1.2

2.6

ND

Cmax (ng/mL)

 

177

 

113 ± 22.4

Tmax (h)

 

2.00

 

2.00

AUC0-last (ng.h/mL)

767

568

352 ± 30.6

453 ± 89.3

AUC0-inf (ng.h/mL)

772

577

372 ± 43.3

487 ± 102

t1/2 (h)

4.22

4.55

6.21 ± 1.65

6.64 ± 1.41

Vss (L/kg)

6.53

 

35.6 ± 1.30

 

CL (mL/min/kg)

43.2

 

90.5 ± 10.5

 

Fa*Fg (%)

 

ND

 

80.7

F (%)

 

15.0

 

26.2 ± 5.45

  1. Values reported as mean, n = 9/group, n = 3/timepoint for mouse and mean ± SD, n = 3/group, for rat. PK data analysis was performed using noncompartmental analysis and WinNonlin Phoenix 6.2 (or higher). ND: Not determined.
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