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r-RGD-hirudin
- Development stage
- Unknown
- Lead developer
- Fudan University
- Modality
- Recombinant Proteins and Enzymes, Peptides
- Administration
- Intravenous
01
Overview
r-RGD-hirudin is a novel recombinant bi-functional protein engineered by fusing the Arg-Gly-Asp (RGD) adhesion motif to wild-type hirudin. Hirudins are potent and specific direct thrombin inhibitors originally derived from the medicinal leech (*Hirudo medicinalis*). The addition of the RGD sequence enables this molecule to not only inhibit thrombin-mediated conversion of fibrinogen to fibrin (anticoagulant effect), but also bind platelet glycoprotein IIb/IIIa receptors and inhibit platelet aggregation. This dual mechanism makes r-RGD-hirudin two to three times more effective than wild-type hirudins in preventing thrombosis at lower doses. It is produced recombinantly in *Pichia pastoris* yeast expression systems. Clinical development has focused on intravenous administration for prevention or treatment of thromboembolic disorders[2][5][1].
- Other names
- recombinant bifunctional hirudinBFHRGD-hirudin
02
Targets
GPIIb/IIIa (Integrin alpha-IIb/beta-3)F2 (Thrombin)
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