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Titolo:
Lotrafiban: an oral platelet glycoprotein IIb/IIIa blocker
Autore:
Liu, FQ; Craft, RM; Morris, SA; Carroll, RC;
Indirizzi:
Univ Tennessee, Grad Sch Med, Dept Anesthesiol, Knoxville, TN 37920 USA Univ Tennessee Knoxville TN USA 37920 nesthesiol, Knoxville, TN 37920 USA
Titolo Testata:
EXPERT OPINION ON INVESTIGATIONAL DRUGS
fascicolo: 11, volume: 9, anno: 2000,
pagine: 2673 - 2687
SICI:
1354-3784(200011)9:11<2673:LAOPGI>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
FIBRINOGEN RECEPTOR ANTAGONIST; ACUTE CORONARY SYNDROMES; ASPARTIC ACID RGD; RANDOMIZED TRIAL; IIB-IIIA; GPIIB/IIIA ANTAGONISTS; MYOCARDIAL-INFARCTION; INTEGRIN ANTAGONISTS; AGGREGATION; POTENT;
Keywords:
acute ischaemic syndrome; angioplasty; blocker; myocardial infarction; platelet aggregation; platelet glycoprotein IIb/IIIa receptor; stroke; thrombosis;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
67
Recensione:
Indirizzi per estratti:
Indirizzo: Carroll, RC Univ Tennessee, Grad Sch Med, Dept Anesthesiol, 1924 Alcoa Highway, Knoxville, TN 37920 USA Univ Tennessee 1924 Alcoa Highway Knoxville TN USA 37920 0 USA
Citazione:
F.Q. Liu et al., "Lotrafiban: an oral platelet glycoprotein IIb/IIIa blocker", EXPERT OP I, 9(11), 2000, pp. 2673-2687

Abstract

Platelets play a major role in thrombus formation, as well as in the pathogenesis of atherothrombosis. Inhibition of platelet function is now emphasised more than ever for prevention and treatment of almost all vascular diseases, since thrombosis is established as the key pathogenic event causing acute ischaemic coronary and cerebrovascular syndromes. Although acetylsalicylic acid (aspirin) has been shown to reduce the incidence of myocardial infarction and stroke, its effect is weak and more effective antithrombotic agents are required to manage patients at high-risk for recurrent vascular events. Platelet glycoprotein IIb/IIIa receptor (GPIIb/IIIa) blockade represents a significant advance in interventional cardiology and treatment of acute ischaemic syndromes. The past several years have seen the introduction of many platelet GPIIb/IIIa blockers into the clinical arena targeting the unique platelet GPIIb/IIIa receptor for the adhesive proteins, fibrinogen and von Willebrand Factor. Platelet GPIIb/IIIa blockers administered intravenously have proven efficacious in mitigating arterial thrombosis in acute coronary syndromes (unstable angina and non-ST-elevation myocardial infarction) and percutaneous coronary interventions (PCI) such as balloon dilatation and stent implantation. Currently, orally-active platelet GPIIb/IIIa blockers are being developed to provide additional benefits for primary and secondary prevention of thrombosis as chronic treatment, especially in high-risk patients. Lotrafiban (SmithKline Beecham) is a member of the latest generation of orally-active platelet GPIIb/IIIa blockers undergoing Phase III clinical trials to test the relative effectiveness versus other oral platelet inhibitors for ischaemic conditions including unstable angina, restenosisafter PCI and stroke. Lotrafiban is converted from an esterified prodrug by plasma and liver esterases to a peptidomimetic of the arginine-glycine-aspartic acid amino acid sequence. This sequence itself mimics the binding site of fibrinogen and von Willebrand Factor to the platelet GPIIb/IIIa receptor. Preliminary results of the clinical trial APLAUD (antiplarelet useful dose) show that lotrafiban is clinically safe and well-tolerated in patients with recent myocardial infarction, unstable angina, transient ischaemic attack (TIA), or stroke when added to aspirin therapy. With lotrafiban, a worldwide large-scale Phase III clinical trial BRAVO (blockage of the GPIIb/IIIa receptor to avoid Vascular occlusion) is currently underway. In general, GPIlb/IIIa blockade seems clinically very promising. A number of unresolved issues, however, remain to be elucidated.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/12/20 alle ore 22:42:41