Table 1.

Representative small peptidomimetic inhibitors of FXIa with their inhibitory profiles.

Class	Inhibitor	Inhibition measures	APTT×2	Positive results in models	Ref.
Acyclic
Phenylalanines	18	FXIa Ki = 0.3 nM P.K. Ki = 5 nM	1.0 μMh 2.0 μMrab	1) Arteriovenous-shunt thrombosis model (rabbit) (ID50 = 0.6 mg/kg + 1 mg/kg/h)	48
α-Ketothiazoles	28	FXIa IC50 = 6 nM P.K. IC50= 10 nM	2.4 μMh	1) Venous thrombosis model (rat) (0.25 mg/kg)	52
Moncyclic
Azetidinones	30	FXIa IC50 = 2.8 nM P.K. IC50= 550 nM	0.14 μMh 2.2 μMrat 10.6 μMrab	1) FeCl3-induced thrombosis in both the vena cava and carotid artery models (rat) (0.2 mg/kg+ 0.2 mg/kg/h) 2) Several bleeding tests (rat) 3) Arteriovenous-shunt thrombosis, venous thrombosis, electrolytic-mediated carotid arterial thrombosis models (rabbit) (ED50 = 0.4 – 1.5 mg/kg/h) 4) Cuticle bleeding test (rabbit)	33&34
Bicyclic
Tetrahydroqunolines	47	FXIa Ki = 0.2 nM P.K. Ki = 5 nM	2.2 μMrat 2.4 μMrat	1) Arteriovenous shunt thrombosis model (rabbit) (ID50 = 0.95 mg/kg + 0.6 mg/kg/h) 2) Electrolytic-induced carotid arterial thrombosis (rabbit) (0.37 mg/kg + 0.27 mg/kg/h) 3) Cuticle bleeding test (rabbit)	72