TABLE 3

Quantitation of varenicline and major metabolites in excreta of mice, rats, monkeys, and humans after oral administration of [14C]varenicline


Metabolite (M + H+ ion)

Mouse

Rat

Monkey

Human
% of dose
M1 (amino acid metabolite; m/z 244) 0.53 0.86 1.1 N.D.
M2 (amino acid metabolite; m/z 244) 0.97 0.72 4.3 N.D.
M3 unknown (m/z 338) N.D. 0.95 N.D. N.D.
M3a unknown 0.12 N.D. 1.1 N.D.
M3b (2-hydroxyvarenicline; m/z 228) N.D. N.D. N.D. 2.9
Varenicline (m/z 212) 90 84 75 81
M4 (varenicline N-carbamoylglucuronide; m/z 432)
N.D.
1.9
3.6
3.6
  • N.D. not detected.