Abciximab(Synonyms: C7E3) 目录号 : GC65597
Abciximab (C7E3) 是一种小鼠/人嵌合单克隆抗体，是一种糖蛋白 IIb/IIIa（glycoprotein IIb/IIIa）抑制剂。 Abciximab 通过与糖蛋白 IIb/IIIa、vitronectin 和 Mac-1 受体结合抑制血小板聚集和白细胞粘附。
Sample solution is provided at 25 µL, 10mM.
Abciximab (C7E3), a chimeric mouse/human monoclonal antibody, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.
Abciximab (C7E3) inhibits platelet aggregation induced by physiologic and pathologic agonists by binding to the platelet αIIbβ3 integrin.Abciximab appears to have similar affinity for the αIIbβ3 and αvβ3 integrins and redistributes between them.
Abciximab (C7E3) (0.25 mg/kg/day; i.v.; 28 days) effectively prevents neointimal hyperplasia.
. Ibbotson T, et al. Abciximab: an updated review of its therapeutic use in patients with ischaemic heart disease undergoing percutaneous coronary revascularisation. Drugs. 2003;63(11):1121-63.
. Wu CH, et al. Mechanisms involved in the inhibition of neointimal hyperplasia by abciximab in a rat model of balloon angioplasty. Thromb Res. 2001 Feb 1;101(3):127-38.
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How Abciximab might be clinically useful
Int J Cardiol 2016 Nov 1;222:1074-1078.PMID:27519521DOI:10.1016/j.ijcard.2016.07.213.
Platelet aggregation is a crucial feature in coronary artery thrombus formation and is a major causative factor in both acute coronary syndromes (ACS) and reocclusion after percutaneous coronary interventions (PCI). The glycoprotein (GP) IIb/IIIa (αIIbβ3) integrin receptor is the pivotal mediator of platelet aggregation. In late 1990s, the introduction of GP IIb/IIIa inhibitors (GPI) was associated with a reduction of ischemic complication, and a clear clinical benefit in PCI during ACS, for both non ST-elevation (NSTE) and ST-segment elevation myocardial infarction (STEMI). The currently available GPI (Abciximab, eptifibatide and tirofiban) tended to be replaced in the current therapy of STEMI by different agents and this is in part related to the effectiveness and to the potential adverse effects (thrombocytopenia and bleeding). There might be a certain level of variability among these agents and here we have reviewed only Abciximab in detail. Interestingly, however, the story may not be entirely different from that of positive inotropic agents in the context of acute ischemia where the potent action to sustain left ventricular function had an arrhythmogenic counterpart to evaluate and take into consideration and therefore therapeutically it will always be necessary to weigh benefits and harms if actions are expected by relatively potent agents.
Abciximab as an adjunctive therapy for patients undergoing percutaneous coronary interventions
Expert Opin Biol Ther 2011 Feb;11(2):235-46.PMID:21204736DOI:10.1517/14712598.2011.551113.
Introduction: Platelets play a central role in the pathophysiology of acute coronary syndromes (ACS) and activation of platelet glycoprotein (GP) IIb/IIIa receptor is critical to platelet aggregation. Abciximab, a human murine chimeric antibody to the GPIIb/IIIa receptor, is an important biological therapy in the management of patients presenting with ACS. Areas covered: The objective of this review is to define the role of Abciximab in the management of ACS by interpreting the available data from randomized clinical trials using Abciximab in various clinical scenarios, particularly in percutaneous coronary intervention (PCI). We also review different modes of delivery and describe the adverse effects of Abciximab including thrombocytopenia. Where possible, we attempt to compare Abciximab to the other available GPIIb/IIIa inhibitors. We hope the reader will gain a better understanding of the benefits and risks of Abciximab and the important role it has in the management of cardiology patients. Expert opinion: Abciximab was a breakthrough drug in the management of high risk ACS patients undergoing PCI. However, with newer available therapies and improvement in PCI technology, dose and delivery of this drug have evolved as we try to extract maximum benefit while minimizing the adverse effects associated with it.
Abciximab: a new antiaggregant used in angioplasty
Ann Pharmacother 1996 Mar;30(3):251-7.PMID:8833561DOI:10.1177/106002809603000309.
Objective: To review the scientific literature on the pharmacology and clinical uses of Abciximab. Data sources: MEDLINE, Index Medicus, and bibliographic literature searches of English-language articles pertaining to Abciximab, 7E3, m7E3, and c7E3 were performed. Eli Lilly also provided unpublished results of the Evaluation of 7E3 for the Prevention of Ischemic Complications trial. Data selection: The selection of data presented focused on controlled trials using Abciximab at doses currently approved by the Food and Drug Administration. Data synthesis: Abciximab is a humanized chimeric Fab fragment of 7E3. 7E3 is a murine antibody directed against the integrin glycoprotein IIb)/IIIa receptor (GPIIb/IIIa) located on platelets. These receptors play an integral part in platelet aggregation by allowing fibrinogen to bind to them and interconnect platelets. When administered intravenously, Abciximab binds to GPIIb/IIIa and hinders platelet aggregation. Bleeding times and activated clotting times are increased and the platelets' response to adenosine diphosphate is reduced with the use of Abciximab. Clinical trials have indicated that Abciximab can reduce the incidence of abrupt closure and restenosis associated with percutaneous transluminal coronary angioplasty (PTCA) performed in high-risk patients. Clinical trials also suggest that Abciximab may have a role in the treatment of unstable angina and the acute therapy of myocardial infarctions. Complications associated with Abciximab include bleeding and thrombocytopenia. The thrombocytopenia is likely related to immunologic mechanisms. In addition, the production of antimurine antibodies has been demonstrated with Abciximab use. Abciximab is currently approved for the prevention of abrupt coronary closure associated with PTCA in patients at high risk for this event. Conclusions: Abciximab is effective in preventing platelet aggregation and has been proven to be of clinical benefit in selected high-risk patients receiving PTCA.
Abciximab. A pharmacoeconomic review of its use in percutaneous coronary revascularisation
Pharmacoeconomics 1999 Dec;16(6):711-41.PMID:10724797DOI:10.2165/00019053-199916060-00009.
Abciximab is a monoclonal antibody fragment that inhibits platelet aggregation through antagonism of glycoprotein IIb/IIIa. The drug is used in conjunction with heparin and aspirin to prevent ischaemic complications associated with percutaneous coronary revascularisation in patients with coronary heart disease. Large and well designed clinical studies have shown Abciximab, as an adjunct to aspirin and heparin, to reduce by around one-third to one-half the incidence of ischaemic complications within 30 days of percutaneous coronary revascularisation. Use of the drug appears advantageous in patients at high risk, and Abciximab also reduces complications in patients undergoing coronary stenting, although the drug does not appear to inhibit restenotic tissue volume within stents. Longer term benefit has also been reported, with emerging 1-year data from a study in patients at all levels of risk showing reductions in a composite end-point of death, myocardial infarction (MI) or urgent repeat revascularisation. Three-year benefit has been reported in high risk patients. Meta-analysis results, and 1-year data from patients receiving stents, have shown reduced mortality with Abciximab. Abciximab therapy had an incremental cost over standard therapy from a hospital perspective of $US293 per patient (1991/1992 values) over 6 months in a prospective economic substudy from a major US clinical trial of the drug in high risk patients. Abciximab was cost saving in patients with unstable angina. A mean net cost of hospitalisation of $US476 per patients (1995 costs) has been shown in a further study in patients with a broad range of levels of risk, and observational data indicate reduced duration of hospitalisation with Abciximab. Cost-effectiveness data favoured Abciximab with aspirin and heparin over a 6-month period in Spanish and Dutch analyses in which data from the above trial were combined with local cost data, but not in an Australian analysis. Subgroup analyses have indicated enhanced cost effectiveness in high risk patients. Available data also show clinical benefit and cost effectiveness of Abciximab therapy in conjunction with coronary stent placement. Conclusions: Data indicate intravenous bolus plus 12-hour infusion regimens of Abciximab to be economically viable in patients at high or low risk of ischaemic complications after percutaneous coronary revascularisation. The drug has been shown to be cost effective in patients receiving the drug in conjunction with coronary stents, and subgroup analyses indicate additional cost effectiveness in certain groups of patients at high risk of ischaemic complications (notably those with acute MI and unstable angina).
Delayed thrombocytopenia following administration of Abciximab: Pharmacovigilance survey and literature review
Therapie 2021 Nov-Dec;76(6):687-693.PMID:33726948DOI:10.1016/j.therap.2021.02.006.
Background: Abciximab (ABX) is used for acute coronary syndrome and unstable angina. Thrombocytopenia is a frequent adverse effect described as occurring in the first 24hours. The aim of this study was to evaluate, in a context of pharmacovigilance survey, the occurrence of delayed thrombocytopenia following ABX infusion in pharmacovigilance database reports and in the literature. Methods: Individual case safety reports (ICSRs) of delayed thrombocytopenia-between 3 and 30 days - with ABX presented as a single suspect were selected in VigiBase®, the WHO global database of ICSRs. The French cases were then extracted from the French national pharmacovigilance database. In addition, a literature review of published cases was performed using PubMed. Results: Among the 84 ICSRs selected from VigiBase®, 43 were also reported in the FPVD. Mean age was 60.1±12.3 years with a majority of male patients (77.4%). The average time to onset (TTO) was 8.9±5.2 days. Thrombocytopenia regressed in 5.1±2.7 days. Haemorrhagic complications were reported in 15% of ICSRs. In the French cases, the median nadir of platelet count was 28×109/L (range 1-110) with a majority of grade 4 thrombocytopenia (39.5%). The literature review identified 42 cases and provided additional information on administered therapies, which include platelet units, corticosteroids, and IV immunoglobulins. GPIIb/IIIa-ABX complex antibodies were described in 26 published cases. Conclusion: Delayed thrombocytopenia, probably due to immune reaction, is a possible life-threatening adverse effect of ABX with a mean TTO of 9 days, supporting the recommendation of a platelet count monitoring during at least two weeks. This recommendation was added to the abcximab SmPC in 2019.