TABLE 4

Mean (n = 6 for urine and n = 5 for feces) percentage dose excreted in urine and feces identified as semagacestat and metabolites from healthy male human subjects after a single 140-mg oral dose of [14C]semagacestat dihydrate

Peak% of the Dose
UrineFecesTotal
Parent44.12 ± 5.890.52 ± 0.6344.55 ± 5.87
M38.58 ± 1.771.12 ± 1.119.51 ± 2.06
M27.58 ± 2.040.65 ± 0.488.12 ± 2.35
M305.95 ± 1.15N.D.5.95 ± 1.15
M4 + M53.64 ± 0.550.62 ± 0.284.16 ± 0.74
M212.28 ± 1.160.34 ± 0.272.57 ± 1.26
M25 + M33a2.50 ± 1.04Trace2.50 ± 1.04
M22 + M31b1.86 ± 1.220.22 ± 0.262.05 ± 1.12
M8 + M201.24 ± 0.400.96 ± 0.622.04 ± 0.88
M191.45 ± 0.510.03 ± 0.061.48 ± 0.53
M60.77 ± 0.500.07 ± 0.100.82 ± 0.54
M70.75 ± 0.470.11 ± 0.170.84 ± 0.54
M12 + M36c0.44 ± 1.020.08 ± 0.170.50 ± 1.01
M11Trace0.39 ± 0.310.33 ± 0.32
M170.22 ± 0.300.06 ± 0.140.28 ± 0.28
M10Trace0.30 ± 0.190.25 ± 0.20
M35N.D.0.30 ± 0.330.25 ± 0.32
M9Trace0.15 ± 0.240.12 ± 0.22
M32Trace0.06 ± 0.090.05 ± 0.09
M34N.D.0.06 ± 0.090.05 ± 0.09
M26N.D.0.02 ± 0.040.02 ± 0.04
  • Trace, only detected by LC/MS; N.D., not detected.

  • a M25 and M33 were coeluted in urine, and M33 was not detected in feces.

  • b M22 and M31 were coeluted, and M31 was not detected in feces.

  • c M12 and M36 were coeluted in feces, and M36 was not detected in urine.