Monitoring direct FXa-inhibitors and fondaparinux by Prothrombinase-induced Clotting Time (PiCT): relation to FXa-activity and influence of assay modifications

Thromb Res. 2008;123(2):396-403. doi: 10.1016/j.thromres.2008.05.010. Epub 2008 Jun 24.

Abstract

Introduction: FXa-activity can be measured by the Prothrombinase induced Clotting time (PiCT). The manufactured assay uses bovine FXa as component and employs a incubation period before re-calcification. Its use with new direct FXa-inhibitors is challenged by reports on decreased sensitivity.

Methods: Blood was incubated with 3 investigational, structurally related (oxazolidinones) direct FXa-inhibitors including the recently approved agent rivaroxaban (0 - 2.0 microM), with the structurally distinct direct FXa-inhibitor DX 9065a (0 - 18 microM) and with the indirect inhibitor fondaparinux (0 - 0.6 microM). We tested modifications of PiCT regarding the source of FXa (bovine or human) and the incubation step (incubation before re-calcification=2-step, no incubation =1-step), and compared results with inhibition of human or bovine FXa-activity.

Results: The bovine 2-step PiCT showed a paradoxical decrease with all direct FXa-inhibitors, this effect is surmounted only at high concentrations and is not seen with the bovine 1-step PiCT. The decrease in PiCT is not observed in antithrombin-depleted plasma. The humanized PiCT (1 or 2 step) showed a consistent prolongation under all direct inhibitors. Fondaparinux prolonged PiCT with either assay. The correlation between PiCT and corresponding FXa-activity was significant both for humanized 2-step PiCT or bovine 1 step PiCT (r2=0.80), but the 95% prediction interval was large and covered a span of 40% FXa-activity between one agent and another.

Conclusions: The customary bovine PiCT should only be used to monitor direct FXa-inhibitors when modified as 1-step procedure. PiCT is not suitable to assess similarity of FXa-inhibition when different agents are interchanged.

MeSH terms

  • Animals
  • Anticoagulants / pharmacology*
  • Antithrombins / pharmacology
  • Biological Assay
  • Blood Coagulation Tests / methods*
  • Cattle
  • Dose-Response Relationship, Drug
  • Drug Monitoring / methods*
  • Factor Xa Inhibitors*
  • Fondaparinux
  • Humans
  • Inhibitory Concentration 50
  • Partial Thromboplastin Time
  • Polysaccharides / pharmacology*
  • Thromboplastin / antagonists & inhibitors
  • Thromboplastin / pharmacology

Substances

  • Anticoagulants
  • Antithrombins
  • Factor Xa Inhibitors
  • Polysaccharides
  • Thromboplastin
  • Fondaparinux