TABLE 1

Changes of serum bile acids after a single intravenous dose of 100 mg/kg of TAK-875 to Sprague-Dawley rats (each group n = 6)

BA typeControlTAK-875
No.(ng/ml)Predose1 hour PostdoseFoldPredose1 hour PostdoseFold
1CAa32,508 ± 16,45327,242 ± 16,6700.870 ± 0.35822,973 ± 10,92674,797 ± 19,2592.94 ± 0.50
2DCA2796 ± 13862650 ± 11400.985 ± 0.3501891 ± 8033308 ± 10501.85 ± 0.43
3UDCAa6654 ± 27155591 ± 29170.846 ± 0.2955710 ± 284414,661 ± 47482.80 ± 0.67
4LCA33.7 ± 13.325.0 ± 5.10.798 ± 0.20930.8 ± 12.325.6 ± 6.80.876 ± 0.155
5GCA1700 ± 7801156 ± 6140.713 ± 0.2981148 ± 10351335 ± 11191.30 ± 0.70
6CDCA4355 ± 8633590 ± 11880.923 ± 0.4504946 ± 29885633 ± 32181.24 ± 0.35
7GDCA415 ± 167303 ± 1410.742 ± 0.198270 ± 151269 ± 1771.02 ± 0.45
8GCDCA127 ± 5794 ± 470.794 ± 0.301139 ± 83181 ± 1061.43 ± 0.71
9GUDCA471 ± 201362 ± 2860.754 ± 0.337330 ± 192404 ± 2321.46 ± 0.82
10TCDCAa79 ± 24110 ± 351.40 ± 0.3199 ± 40281 ± 1372.87 ± 0.62
11TCAa238 ± 105337 ± 1371.45 ± 0.33289 ± 175635 ± 2742.17 ± 0.85
  • a Indicates >2-fold increase at 1 hour postdose compared with the predose.