Abrams Charles S, Cines Douglas B
Hematology-Oncology Division, University of Pennsylvania, 421 Curie Boulevard, Basic Research Building II/III, Room 912, Philadelphia, PA 19104, USA.
Curr Hematol Rep. 2004 Mar;3(2):143-7.
Abciximab, eptifibatide, and tirofiban are the three drugs approved by the US Food and Drug Administration designed to block platelet aggregation by binding glycoprotein IIb/IIIa. Results from large therapeutic trials demonstrate that all three agents induce thrombocytopenia in approximately 1% to 5% of cardiac patients. Thrombocytopenia is typically rapid in onset and antibody mediated. In vitro evidence suggests abciximab-induced thrombocytopenia is associated with antibodies directed to murine sequences within the chimeric anti-IIb/IIIa molecule. In addition, abciximab, eptifibatide, and tirofiban also function as mixed agonist-antagonists in vivo, inducing neoepitopes within the glycoprotein IIb/IIIa receptor that may react with pre-existing or induced antibodies. Screening for the development of these antibodies may reduce the incidence of thrombocytopenia associated with these agents, but it may limit their chronic usage.
阿昔单抗、依替巴肽和替罗非班是美国食品药品监督管理局批准的三种药物，旨在通过结合糖蛋白IIb/IIIa来阻止血小板聚集。大型治疗试验结果表明，这三种药物在大约1%至5%的心脏病患者中会导致血小板减少。血小板减少通常起病迅速且由抗体介导。体外证据表明，阿昔单抗诱导的血小板减少与针对嵌合抗IIb/IIIa分子中鼠源序列的抗体有关。此外，阿昔单抗、依替巴肽和替罗非班在体内还起混合激动剂-拮抗剂的作用，在糖蛋白IIb/IIIa受体内诱导新表位，这些新表位可能与预先存在的或诱导产生的抗体发生反应。筛查这些抗体的产生可能会降低与这些药物相关的血小板减少的发生率，但可能会限制它们的长期使用。
