Intrinsic activating properties of GP IIb/IIIa blockers

Thromb Res. 2001 Sep 30:103 Suppl 1:S21-7. doi: 10.1016/s0049-3848(01)00300-0.

Abstract

Potential intrinsic activating properties are probably the most controversially discussed issues with respect to GP IIb/IIIa blockers, especially since clinical trials with oral GP IIb/IIIa blockers revealed disappointing results. Based on the finding that currently clinically used GP IIb/IIIa blockers are ligand mimetics, experimental data are discussed, demonstrating an intrinsic activating effect of ligand mimetic GP IIb/IIIa blockers that potentially results in fibrinogen binding to alpha(IIb)beta(3) and in platelet aggregation. Furthermore, the inhibitory effect of aspirin on GP IIb/IIIa blocker-induced platelet aggregation is discussed as a clinically relevant finding. Finally, the potential association of GP IIb/IIIa blocker-induced thrombocytopenia with platelet activation is described.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal / metabolism
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal / therapeutic use
  • Humans
  • Oligopeptides / metabolism
  • Oligopeptides / pharmacology
  • Oligopeptides / therapeutic use
  • Platelet Aggregation Inhibitors / metabolism
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Aggregation Inhibitors / therapeutic use
  • Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors*
  • Protein Binding

Substances

  • Antibodies, Monoclonal
  • Oligopeptides
  • Platelet Aggregation Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • arginyl-glycyl-aspartic acid