Table 3 VX-765 and VRT-043198 are detected in the CSF after a single IP dose of VX-765.

From: Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging

Time (h)

Mouse 1 VX-765 (μM)

Mouse 2 VX-765 (μM)

Mouse 1 VRT-043198 (μM)

Mouse 2 VRT-043198 (μM)

Mean VX-765 (μM)(a)

Mean VRT-043198 (μM)(b)

0.25

0.21*

0.45

82.6*

3.11

0.33

42.9

0.50

0.07

1.17

0.44

7.00

0.62

3.72

1

0.06

0.10

0.43

0.58

0.08

0.50

3

0.07*

0.04*

0.42*

0.15*

0.06

0.28

6

0.05*

0.06*

NQ*

0.21*

0.06

0.21

8

0.07*

0.13*

0.13*

0.60*

0.10

0.36

24

NQ

NQ*

NQ

NQ*

−

−

Cmax (μM)(c)

0.21

1.17

82.6

7.00

0.69

44.8

Tmax (h)(d)

0.25

0.50

0.25

0.5

0.38

0.38

Half-life (t1/2) (h)(e)

NC

NC

NR

NC

−

−

MRTinf (h)(f)

NC

NC

0.81

NC

−

0.81

  1. NQ: not quantifiable. No peak of below lower limit of quantification: 0.006 μM for VX-765 and 0.068 μM for VRT-043198.
  2. NC: not calculated due to shape of PK curve.
  3. NR: not reported. The span of the terminal phase is too short to allow for accurate estimation of half-life.
  4. *Some blood contamination during CSF collection.
  5. Individual data points showing VX-765 and VRT-043198 concentrations up to 24 h post-injection (n = 2 per time point). (a) VX-765 and (b) VRT-043198 mean concentrations at each time point. (c) Maximum concentration achieved (Cmax), (d) time to reach Cmax (Tmax), (e) half-life (t1/2) and (f) mean residence time (MRT) in the CSF for VX-765 and VRT-043198.
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