Drug intelligence / Profile preview

pegmusirudin

Development stage
Phase 2
Lead developer
Novartis
Modality
Recombinant Proteins and Enzymes, Peptides, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Subcutaneous
01

Overview

PEG-hirudin (pegmusirudin) is a chemically defined conjugate of recombinant hirudin and two molecules of polyethylene glycol (PEG)-5000. It is a highly selective direct thrombin inhibitor with significantly prolonged duration of action compared to non-conjugated recombinant hirudin, allowing for once-daily subcutaneous administration. The PEGylation reduces the elimination rate and extends the half-life, resulting in prolonged anticoagulant efficacy and improved antithrombotic activity. PEG-hirudin has been investigated for use in indications requiring long-lasting antithrombin activity such as prevention and treatment of thrombotic disorders including graft occlusion, chronic kidney failure (especially in hemodialysis patients), unstable angina, and blood coagulation disorders[1][2][5][7]. Its mechanism involves direct inhibition of thrombin (factor IIa), thereby preventing fibrin formation and platelet activation.

Other names
pegmusirudin
02

Targets

F2 (Thrombin)

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