TABLE 3

Mass-spectral characterization of primary metabolites of saxagliptin identified in human plasma samples after administration of a single oral dose of [14C]saxagliptin to healthy volunteers

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Metabolite[M + H]+Major Fragment IonsMetabolic Pathway(s)
Saxagliptin316180
M1332196Hydroxylation
5-Hydroxy saxagliptin (M2)332196Hydroxylation
M3332196Hydroxylation
M13332304, 196Hydroxylation, cyclization
M16332314, 196Hydroxylation
M45396298, 260Sulfation
M46492474, 316, 298Glucuronidation
D1316288, 180Cyclization