TABLE 7

Cross-species summary of observed versus expected CNS penetration of CP-615,003 and CP-900,725


Compound

Species

CNS Site

Observed Kp

Expected Kpa

Expected/Observed Ratio
CP-615,003 Rat Whole Brain 0.162 2.04 12.6
CSF 0.0102 0.0613 6.0
ECF 0.00143 0.0613 42.9
Dog CSF 0.034 0.267 7.9
Human CSF 0.024 0.233 9.7
CP-900,725 Rat Whole Brain 0.0824 0.903 11.0
CSF 0.0206 0.0569 2.8
ECF 0.0145 0.0569 3.9

Human
CSF
0.0166
0.148
8.9
  • a Expected Kp values for CSF and ECF are the respective fu, plasma values; expected Kp values for whole brain tissue are the respective fu, plasma/fu, brain ratios.