Platelet Protective Effect of TAK-029, A Novel Glycoprotein IIb/IIIa Antagonist: An In Vitro Study

Authors: Kawahito, Koji1; Fujimura, Akio2; Kobayashi, Eiji2; Misawa, Yoshio1; Fuse, Katsuo1

Source: Artificial Organs, Volume 22, Number 4, April 1998 , pp. 348-352(5)

Publisher: Blackwell Publishing

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Abstract:

Previous studies have indicated that exposure of fibrinogen receptors associated with the glycoprotein IIb/IIIa complex contributes to platelet loss during cardiopulmonary bypass. TAK-029 is a newly developed reversible, nonpeptide inhibitor of platelet glycoprotein IIb/IIIa receptors. In this study, we tested the platelet preserving effect of TAK-029 in an in vitro model. The methods included the comparison of the release of β-thromboglobulin (β-TG) between a TAK-029 group (n = 5) and a control group (n = 5) in a mock circulation under a shear force generated by a centrifugal pump. To evaluate the degree of β-TG release, Δβ-TGT was calculated where Δβ-TG is the increase in βTG and ΔT is the time. The results showed that the value of Δβ-TGT in the TAK-029 group was significantly lower than it was in the control group (4.22 ± 0.27 × 102 ng/ml vs. 7.33 ± 0.66 × 102 ng/ml, respectively). In conclusion, TAK-029 reduced the platelet activation under the shear forces of an in vitro model, suggesting that TAK-029 is a potential candidate for platelet protection during cardiopulmonary bypass.

Keywords: Platelet; Glycoprotein IIb/IIIa; Cardiopulmonary bypass

Document Type: Original article

DOI: 10.1046/j.1525-1594.1998.06050.x

Affiliations: 1: Department of Cardiovascular Surgery, Jichi Medical School, Tochigi, Japan 2: Department of Clinical Pharmacology, Jichi Medical School, Tochigi, Japan

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