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Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor.

Publication ,  Journal Article
Ohman, EM; Harrington, RA; Lincoff, AM; Kitt, MM; Kleiman, NS; Tcheng, JE
Published in: Eur Heart J
November 1995

Aggregation of platelets leading to thrombosis is one of the hallmarks of unstable angina, acute myocardial infarction, and ischaemic complications following coronary angioplasty. Activated platelets bind to fibrinogen through the glycoprotein IIb/IIIa integrin receptor. New agents have been developed to bind this receptor and thus prevent aggregation of platelets. One such compound (integrelin) is a cyclical peptide that has been shown to be a potent inhibitor of the glycoprotein IIb/IIIa receptor in man. A number of phase I and phase II clinical trials have been completed to evaluate this agent for the indications of unstable angina, acute myocardial infarction, as well as an adjunct to coronary angioplasty. This article will focus on the clinical investigation of integrelin with particular emphasis on its use during angioplasty. It has been consistently shown across different trials that integrelin can inhibit between 70% and 95% of platelet aggregation responses to 20 mumols of ADP at a variety of dosages used in the phase II trials. Preliminaray data also suggest that a more clinically unstable patient may require a higher dose of integrelin to cause a near complete inhibition of the platelet aggregation response to ADP. Future studies will need to explore more definitely the relationship between dose of glycoprotein IIb/IIIa receptor blockers and clinical instability.

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Published In

Eur Heart J

DOI

ISSN

0195-668X

Publication Date

November 1995

Volume

16 Suppl L

Start / End Page

50 / 55

Location

England

Related Subject Headings

  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Platelet Aggregation Inhibitors
  • Platelet Activation
  • Peptides
  • Humans
  • Eptifibatide
  • Coronary Thrombosis
  • Clinical Trials as Topic
  • Cardiovascular System & Hematology
  • Blood Platelets
 

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Ohman, E. M., Harrington, R. A., Lincoff, A. M., Kitt, M. M., Kleiman, N. S., & Tcheng, J. E. (1995). Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor. Eur Heart J, 16 Suppl L, 50–55. https://doi.org/10.1093/eurheartj/16.suppl_l.50
Ohman, E. M., R. A. Harrington, A. M. Lincoff, M. M. Kitt, N. S. Kleiman, and J. E. Tcheng. “Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor.Eur Heart J 16 Suppl L (November 1995): 50–55. https://doi.org/10.1093/eurheartj/16.suppl_l.50.
Ohman EM, Harrington RA, Lincoff AM, Kitt MM, Kleiman NS, Tcheng JE. Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor. Eur Heart J. 1995 Nov;16 Suppl L:50–5.
Ohman, E. M., et al. “Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor.Eur Heart J, vol. 16 Suppl L, Nov. 1995, pp. 50–55. Pubmed, doi:10.1093/eurheartj/16.suppl_l.50.
Ohman EM, Harrington RA, Lincoff AM, Kitt MM, Kleiman NS, Tcheng JE. Early clinical experience with integrelin, an inhibitor of the platelet glycoprotein IIb/IIIa integrin receptor. Eur Heart J. 1995 Nov;16 Suppl L:50–55.
Journal cover image

Published In

Eur Heart J

DOI

ISSN

0195-668X

Publication Date

November 1995

Volume

16 Suppl L

Start / End Page

50 / 55

Location

England

Related Subject Headings

  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Platelet Aggregation Inhibitors
  • Platelet Activation
  • Peptides
  • Humans
  • Eptifibatide
  • Coronary Thrombosis
  • Clinical Trials as Topic
  • Cardiovascular System & Hematology
  • Blood Platelets