TABLE 2

Estimates of anacetrapib t½ (days) in mouse blood and tissues after 6-week dosing and to 35 weeks postdosing

Anacetrapib was dosed orally once daily to WT-lean, WT-DIO, NFR-lean, and NFR-DIO mice at 10 mg/kg for 42 days. Blood and tissues were collected during dosing and at 4, 12, 16, 24, and 35 weeks postdose. Drug levels were measured by LC-MS/MS as described in Methods. The t½ estimates were calculated from the last three data points of the mean concentration time curves from blood and tissues.

WT LeanWT DIONFR LeanNFR DIO
Blood39125256292
Liver230115125143
Adipose brown94115118145
Adipose whiteNCa171NCa277
Brain574726130
  • a Not calculated: A reliable t½ estimate could not be obtained from these tissues, as the terminal phase could not be determined.