TABLE 3

The composition of conjugative metabolites of motesanib in microsomes across species


Cofactor


Percentage of Metabolite Formationa
Metabolite
Rat
Mouse
Dog
Monkey
Human
UDP-GA M1 20.5 6.6 13.6 28.5 67.7
UDP-glucose Mb 5.1 9.3 3.1 46.2 ND
UDP-N-acetylglucosamine
Mc
ND
ND
ND
24.4
ND
  • ND, not detected.

  • a Results obtained by HPLC with a β-RAM radiometric detector. Percentages represent mean relative amount of conjugative metabolites M1, Mb, and Mc formed in microsomal incubations (n = 2 for each species) using 10 μM motesanib and 1 mg/ml microsomal protein incubated in the presence of cofactor (2 mM) at 37°C for 30 min.