DOI: 10.1161/01.cir.98.11.1085. Abciximab (ReoPro, Chimeric 7E3 Fab) Demonstrates Equivalent Affinity and Functional Blockade of Glycoprotein IIb/IIIa and α <sub>v</sub> β <sub>3</sub> Integrins

Abciximab (ReoPro, Chimeric 7E3 Fab) Demonstrates Equivalent Affinity and Functional Blockade of Glycoprotein IIb/IIIa and α v β 3 Integrins

10.1161/01.cir.98.11.1085

Crossref journal-article

Ovid Technologies (Wolters Kluwer Health)

Circulation (276)

Abstract

Background —Large, randomized, and blinded clinical trials (EPIC, EPILOG, and CAPTURE) have demonstrated that abciximab (ReoPro, chimeric 7E3 Fab) markedly reduces thrombotic events associated with percutaneous transluminal coronary interventions. The marked early benefits at 30 days were sustained at 6 months and 3 years. Initially developed because of its efficacy in blocking GP IIb/IIIa (α IIb /β 3 ) receptors on platelets, abciximab also binds with equivalent affinity to α v β 3 . Methods and Results —This study presents a detailed characterization of the α v β 3 interaction, including the ability of abciximab to (1) bind with comparable affinity to α v β 3 and GP IIb/IIIa, (2) inhibit α v β 3 and GP IIb/IIIa–mediated cell adhesion in vitro with IC 50 values approximating binding K D values, and (3) redistribute between GP IIb/IIIa and α v β 3 integrins in vitro. Conclusions —As an antagonist of not only GP IIb/IIIa but also α v β 3 , abciximab may provide additional clinical benefit in preventing α v β 3 -mediated effects such as thrombin generation, clot retraction, or smooth muscle cell migration and proliferation. Abciximab binds with equivalent affinity to both GP IIb/IIIa and α v β 3 and redistributes between the 2 integrin receptors in vitro. Abciximab has been previously shown to circulate on platelets for up to 2 weeks. Taken together, these findings suggest that abciximab may have the ability to inhibit both GP IIb/IIIa and α v β 3 for extended periods.

Bibliography

Tam, S. H., Sassoli, P. M., Jordan, R. E., & Nakada, M. T. (1998). Abciximab (ReoPro, Chimeric 7E3 Fab) Demonstrates Equivalent Affinity and Functional Blockade of Glycoprotein IIb/IIIa and Î± v Î² 3 Integrins. Circulation, 98(11), 1085â1091.

Authors 4

Susan H. Tam (first)
Patricia M. Sassoli (additional)
Robert E. Jordan (additional)
Marian T. Nakada (additional)

References 34 Referenced 183

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Jordan RE, Wagner CL, Gray JW, Bhattacharya S, Sane DC, Machin SJ, Mackie I, Anderson KM, Mattis JA, Weisman HF. Molecular pharmacology of chimeric 7E3 monoclonal Fab fragment in human subjects: Plasma clearance and binding to platelet GP IIb/IIIa receptors. Blood. 1991;78:489A. Abstract.Abciximab has comparable affinity and blocking efficacy for αvβ3 and GP IIb/IIIa in vitro. Abciximab also redistributes in vitro between GP IIb/IIIa and αvβ3 integrins. As an antagonist of both GP IIb/IIIa and αvβ3, abciximab may offer added clinical benefit by preventing αvβ3-mediated effects such as thrombin generation, clot retraction, or smooth muscle cell migration and proliferation. Abciximab has been previously shown to circulate on platelets for up to 2 weeks. These findings suggest that abciximab may continue to inhibit both GP IIb/IIIa and αvβ3 after therapy has ceased. / Blood (1991)

Dates

Type	When
Created	13 years, 2 months ago (June 11, 2012, 8:41 p.m.)
Deposited	1 year, 3 months ago (May 12, 2024, 12:19 p.m.)
Indexed	5 days, 23 hours ago (Aug. 31, 2025, 6:28 a.m.)
Issued	26 years, 11 months ago (Sept. 15, 1998)
Published	26 years, 11 months ago (Sept. 15, 1998)
Published Print	26 years, 11 months ago (Sept. 15, 1998)

Funders 0

None

BibTeX

@article{Tam_1998, title={Abciximab (ReoPro, Chimeric 7E3 Fab) Demonstrates Equivalent Affinity and Functional Blockade of Glycoprotein IIb/IIIa and α v β 3 Integrins}, volume={98}, ISSN={1524-4539}, url={http://dx.doi.org/10.1161/01.cir.98.11.1085}, DOI={10.1161/01.cir.98.11.1085}, number={11}, journal={Circulation}, publisher={Ovid Technologies (Wolters Kluwer Health)}, author={Tam, Susan H. and Sassoli, Patricia M. and Jordan, Robert E. and Nakada, Marian T.}, year={1998}, month=sep, pages={1085–1091} }

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