BMC Pharmacology

Table 5 Maximum levels of inhibition of human and monkey plasma DPP activity using ala-pro-AFC as substrate

From: Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

	Rhesus		Cyno		Human
	IC₅₀ (nM)	Max % inhib	IC₅₀ (nM)	Max % inhib	IC₅₀ (nM)	Max % inhib
saxagliptin	2.9 ± 0.3	86 ± 1^†††	2.4 ± 0.2	81 ± 6^††	4.0 ± 0.8	100 ± 0
vildagliptin	17 ± 5**	85 ± 1^†††	13 ± 4**	79 ± 6^††	20 ± 7*	98 ± 1
sitagliptin	17 ± 2***	87 ± 1^†††	17 ± 2***	80 ± 7^††	22 ± 3***	98 ± 0

N = 3 independent experiments. *P < 0.05, **P < 0.01, ***P < 0.001 versus saxagliptin. ^††P < 0.01, ^†††P < 0.001 versus human

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