Alfimeprase: a novel recombinant direct-acting fibrinolytic.

Abstract

Alfimeprase is a recombinant, direct-acting fibrinolytic zinc metalloprotease. Alfimeprase has direct proteolytic activity primarily against the fibrin(ogen) Aalpha chain. Alfimeprase is covalently bound and neutralised by serum alpha(2)-macroglobulin, a prevalent mammalian protease inhibitor. Preclinical pharmacology studies have shown that fibrinolysis with alfimeprase is up to sixfold more rapid than with select plasminogen activators, such as tissue-type plasminogen activator and urokinase. Alfimeprase directly delivered to a site of thrombosis has the potential to be a fast and effective fibrinolytic, which does not generate the systemic lytic state seen with plasminogen activators that is associated with major bleeding, including intracerebral haemorrhage. Phase I and II studies in individuals with arterial or venous thrombotic events indicate that alfimeprase is active and generally well tolerated.

• Authors: Steven R Deitcher, Walter D Funk, James Buchanan, Shouchun Liu, Michael D Levy, Christopher F Toombs
• Journal: Expert opinion on biological therapy (Expert Opin Biol Ther) Vol. 6 Issue 12 Pg. 1361-9 (Dec 2006) ISSN: 1744-7682 [Electronic] England
• PMID: 17223743 (Publication Type: Journal Article, Review)

Chemical References

• Drugs, Investigational
• Fibrinolytic Agents
• Recombinant Proteins
• Metalloendopeptidases
• alfimeprase

Topics

• Animals
• Drugs, Investigational (pharmacology, therapeutic use)
• Fibrinolytic Agents (pharmacology, therapeutic use)
• Humans
• Metalloendopeptidases (pharmacology, therapeutic use)
• Recombinant Proteins (pharmacology, therapeutic use)