Tirofiban (Aggrastat®)

Cook, Jacquelynn J.; Bednář, Bohumil; Lynch, Joseph J.; Gould, Robert J.; Egbertson, Melissa S.; Halczenko, Wasyl; Duggan, Mark E.; Hartman, George D.; Lo, Mimi; Murphy, Gail; Deckelbaum, Lawrence I.; and, Frederick L. Sax; Barr, Eliav

doi:10.1111/j.1527-3466.1999.tb00015.x

Cited by 39 publications

(14 citation statements)

References 48 publications

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“…Abciximab, the Fab fragment of a chimeric mouse-human monoclonal antibody to αIIbβ3, was the first integrin antagonist in clinical medicine 36 . Two additional parenteral, non-antibody αIIbβ3 antagonists, Eptifibatide 37 and Tirofiban 38 , quickly followed for similar indications, and all three drugs work by directly blocking ligand binding to αIIbβ3. As knowledge pertaining to mechanisms of αIIbβ3 signaling has increased in recent years, therapeutic blockade of specific intracellular facets of inside-out and/or outside-in αIIbβ3 signaling remains an appealing, if only theoretical, possibility 39 .…”

Section: Platelet Integrinsmentioning

confidence: 99%

See 1 more Smart Citation

Integrin-based therapeutics: biological basis, clinical use and new drugs

Ley

Rivera–Nieves

Sandborn

et al. 2016

Nat Rev Drug Discov

335

296

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Integrins are activatable adhesion and signaling molecules. Of the 24 known human integrins, three are currently targeted therapeutically by monoclonal antibodies, peptides or small molecules. The platelet αIIbβ3 integrin is targeted by Abciximab, Eptifibatide and Tirofiban, all with indications for preventing thrombotic complications after percutaneous coronary interventions. The lymphocyte α4β1 and α4β7 integrins are targeted by Natalizumab with indications in multiple sclerosis and Crohn’s disease. Although efficacious, use of this antibody is limited by a rare but serious complication, progressive multifocal leukoencephalopathy. Vedolizumab is an antibody to a combinatorial epitope in α4β7 that is approved for use in patients with Crohn’s disease or ulcerative colitis in the United States, Canada and Europe. Progressive multifocal leukoencephalopathy has not been observed in the clinical trials or clinical use of vedolizumab. New antibodies and small molecules targeting β7 integrins (α4β7 and αEβ7) and MAdCAM-1 are in clinical development for treatment of these inflammatory bowel diseases. Overall, integrin-based therapeutics have shown clinically significant benefits in many patients, leading to continued medical interest in the further development of novel integrin inhibitors. Of note, almost all integrin antagonists in use or in late-stage clinical trials target the ligand binding site, or the ligand itself.

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Section: Platelet Integrinsmentioning

confidence: 99%

“…Tirofiban is a highly selective small molecule (N(butylsulfonyl)-O-(4-(4-piperidinyl)butyl)-L-tyrosine monohydrochloride monohydrate) inhibitor of αIIbβ3 that was approved for human use in 1999 38, 44 . Like Eptifibatide, it is highly selective for αIIbβ3 and blocks ADP-induced platelet aggregation.…”

Section: αIibβ3 In Cardiovascular Medicinementioning

confidence: 99%

Integrin-based therapeutics: biological basis, clinical use and new drugs

Ley

Rivera–Nieves

Sandborn

et al. 2016

Nat Rev Drug Discov

335

296

View full text Add to dashboard Cite

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“…NSTEMI was diagnosed if TNI levels were three or more times above normal limit in the absence of ST elevation on ECG [4,8]. In the patients presenting with acute myocardial infarction who were treated with primary angioplasty, re-infarction was defined as the presence of recurrent ischemic symptoms or ECG changes accompanied by a TNI level that was more than five times the upper normal limit or more than 50% higher than the previous value obtained during hospitalization [1][2][3][4][5][6][7][8].…”

Section: Endpointsmentioning

confidence: 99%

Comparison of abciximab with “high-dose” tirofiban in patients undergoing percutaneous coronary intervention

Gunasekara¹,

Walters²,

Aroney³

2006

International Journal of Cardiology

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“…The use of tirofiban (10 g/kg bolus followed by a 0.15 g/kg/min infusion) during PCI has been evaluated in two large multicenter trials with controversial results [2][3][4]. It has recently been suggested that the lack of a more protective clinical response is due to the subtherapeutic inhibition of GP IIb/ IIIa binding activity in these patients [5,6], and this has led to the suggestion of using a bolus dose of 25 g/kg followed by an 18-hr infusion of 0.15 g/kg/min in order to obtain higher blood tirofiban concentrations soon after the start of treatment [7].…”

Section: Introductionmentioning

confidence: 99%

Safety of a high bolus dose of tirofiban in patients undergoing coronary stent placement

Danzi

Capuano

Sesana

et al. 2004

Cathet Cardio Intervent

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To overcome the suboptimal platelet inhibition induced by tirofiban in the first hour after a percutaneous coronary intervention, a new regimen of 25 microg/kg bolus followed by an 18-hr infusion of 0.15 microg/kg/min has been proposed. The aim of this study was to compare the effects of this high bolus dose of tirofiban with those of abciximab on bleeding risk and 30-day clinical outcome in patients undergoing coronary stenting. We compared two cohorts of patients who underwent coronary stent placement between January 2000 and December 2002. In the first cohort, the only available IIb/IIIa receptor inhibitor was abciximab, which was given to 280 (34.9%) out of 802 stented patients; in the second cohort, tirofiban was administered to 274 (38.3%) out of 716 treated patients. The primary endpoints were the proportion of patients with major bleeding and the rate of site access complications; the 30-day incidence of major adverse cardiac events (MACE) was also assessed. After the procedure, the patients were given ticlopidine for 4 weeks and aspirin indefinitely. Major bleeding episodes were observed in four patients receiving abciximab and in none receiving tirofiban (1.4% vs. 0%; P = 0.12); the rates of site access complications were similar (3.6% vs. 3.3%; P = 0.96). The 30-day incidence of MACE was 7.1% in the abciximab group and 5.8% in the tirofiban group (P = 0.65). In patients undergoing coronary stenting, the high bolus dose of tirofiban is safe and not associated with an increased risk of major bleeding or site access complications in comparison with abciximab.

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Tirofiban (Aggrastat®)

Cited by 39 publications

References 48 publications

Integrin-based therapeutics: biological basis, clinical use and new drugs

Integrin-based therapeutics: biological basis, clinical use and new drugs

Comparison of abciximab with “high-dose” tirofiban in patients undergoing percutaneous coronary intervention

Safety of a high bolus dose of tirofiban in patients undergoing coronary stent placement

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