TABLE 3

BMS-423526-induced total cholesterol lowering and tissue levels of drug in guinea pig


BMS-423526 Dose

TC ± S.D.a

TC Percent Loweringb

Drug Levels
Plasma
Liver
Muscle
Mean ± S.D. (Ratio)c
Mean ± S.D. (Ratio)
Mean ± S.D. (Ratio)
nM
0 mg/kg 47.8 ± 3.6
0.25 mg/kg 30.5 ± 9.5 36.1 618 ± 135 (1) 1346 ± 596 (2.2) 49 ± 13 (0.08)
0.5 mg/kg 25.5 ± 2.1 46.6 1227 ± 289 (1) 2352 ± 629 (1.9) 88 ± 25 (0.07)
1.0 mg/kg 20.5 ± 8.9 57.1 3363 ± 489 (1) 4347 ± 849 (1.3) 178 ± 38 (0.05)
1.5 mg/kg 22.9 ± 5.1 52.1 4213 ± 2075 (1) 6261 ± 1518 (1.5) 182 ± 59 (0.04)
2.0 mg/kg
24.0 ± 10.7
49.7
4643 ± 958 (1)
8771 ± 1895 (1.9)
416 ± 125 (0.09)
  • a n = 8 per group; mean plasma TC values in milligram/deciliter.

  • b Relative to vehicle mean.

  • c Relative to mean plasma drug level set to one.