In vitro and ex vivo Activities of CY216: Comparison with Other Low Molecular Weight Heparins

Low molecular weight (LMW) heparins achieve their anticoagulant effects by inhibiting prothrombin activation, catalyzing endogenous thrombin inhibition, and binding thrombin. The extent of which each of the three actions of LMW heparins contributes to the antithrombotic effectiveness of LMW in man has not been defined. Several studies have reported that ex vivo anti-factor Xa activities of LMW heparins correlate with efficacy and potential haemorrhagic complications. However, critical review of the data suggests that anti-factor Xa assays are basically surrogate tests for the mass of LMW heparins in patients' plasmas rather than reliable estimates of total catalytic concentrations of LMW heparins. Antithrombotic effectiveness of LMW heparins probably reflects their ability to inhibit coagulation in vivo. If the last concept proves correct, then results of tests which directly assess the extents to which LMW heparins have suppressed in vivo coagulation may provide more reliable markers for their antithrombotic effectiveness or lack thereof.