Table 1.

Aptamers Isolated Against Coagulation Proteins

Target	DNA/RNA	Binding (Kd)	In vitro activity	In vivo activity	Clinical studies	References
Prothrombin (FII)	RNA	10 μM	Prolongs PT, aPTT, TCT Inhibits platelet activation			[38,58]
Thrombin (FIIa)	DNA	25–200 nM	Prolongs PT	Prolongs PT and ACT in monkeys and canines		[40,41,39,59]
	RNA	2.8 nM	Prolongs clotting time			[42]
	Bivalent RNA	1.3 nM	Prolongs PT and aPTT			[44]
FVII	RNA	59–66 nM	Prolongs PT			[37]
FIX/FIXa	RNA	0.6 nM	Prolongs PT and ACT	Increased bleeding in murine and porcine models with durable reversal with antidote. Patent circuit in porcine bypass	Phase 1A, 1B, 2A and 2B studies demonstrating increased aPTT with return to baseline following antidote administration; safety in cardiac catheterization and PCI; no significant bleeding with sheath removal	[19,20,23–26,28–30,60–62]
FX	RNA	4.4 nM	Prolongs PT and aPTT			[37]
	Bivalent RNA	1.7 nM	Prolongs PT and aPTT			[44]
FXII	RNA	8.9 nM	Prolongs aPTT and TCT			[44]

ACT, activated clotting time; aPTT, activated partial thromboplastin time; PCI, percutaneous coronary intervention; PT, prothrombin time; TCT, thrombin clot time.