Alfimeprase

Identification

Name
Alfimeprase
Accession Number
DB04919
Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description

Alfimeprase is a recombinant analog of fibrolase. Fibrolase is a zinc-containing metalloproteinase isolated from the venom of the southern copperhead snake (Agkistrodon contortrix contortrix). It is a small protein that contains 203 residues (Randolph et al. 1992). Alfimeprase is being developed by Nuvelo.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
>Alfimeprase Sequence
SFPQRYVQLVIVADHRMNTKYNGDSDKIRQWVHQIVNTINEIYRPLNIQFTLVGLEIWSN
QDLITVTSVSHDTLASFGNWRETDLLRRQRHDNAQLLTAIDFDGDTVGLAYVGGMCQLKH
STGVIQDHSAINLLVALTMAHELGHNLGMNHDGNQCHCGANSCVMAAMLSDQPSKLFSDC
SKKDYQTFLTVNNPQCILNKP
Download FASTA Format
Synonyms
Not Available
Categories
UNII
GPN9HBH1HS
CAS number
259074-76-5

Pharmacology

Indication

Alfimeprase is being evaluated as a potential treatment for acute ischemic stroke, catheter occlusion (CO) and acute peripheral arterial occlusion (PAO).

Structured Indications
Not Available
Pharmacodynamics

Alfimeprase is a recombinant direct acting fibrinolytic (rDAF), or blood clot dissolver, that has the potential to rapidly and directly degrade fibrin, a protein that provides the scaffolding for blood clots, when delivered through a catheter to the site of a blood clot.

Mechanism of action

When delivered locally at the site of a blood clot, alfimeprase has the potential, through a unique mechanism of action, to directly and rapidly degrade fibrin, a protein that provides the scaffolding for blood clots. In addition, alfimeprase's thrombolytic activity appears to be localized to the site of delivery because it is rapidly inactivated by alpha-2 macroglobulin, a naturally occurring protein in the blood, as it moves away from the site of delivery and into the general blood circulation.

TargetActionsOrganism
UFibrinogen alpha chainNot AvailableHuman
UFibrinogen beta chainNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Jones G, Ronk M, Mori F, Zhang Z: Disulfide structure of alfimeprase: a recombinant analog of fibrolase. Protein Sci. 2001 Jun;10(6):1264-7. [PubMed:11369866]
External Links
PubChem Substance
347909847

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentArterial Occlusive Diseases / Peripheral Vascular Disease (PVD) / Thrombosis1
2CompletedTreatmentCatheters, Indwelling1
2TerminatedTreatmentAcute Ischemic Stroke (AIS)1
3CompletedTreatmentArterial Occlusive Diseases1
3CompletedTreatmentCatheter Occlusion / Thrombosis / Thrombosis, Venous1
3CompletedTreatmentThrombosis / Thrombosis, Venous1
3TerminatedTreatmentArterial Occlusive Diseases1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Structural molecule activity
Specific Function
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function ...
Gene Name
FGA
Uniprot ID
P02671
Uniprot Name
Fibrinogen alpha chain
Molecular Weight
94972.455 Da
References
  1. Ahmed NK, Tennant KD, Markland FS, Lacz JP: Biochemical characteristics of fibrolase, a fibrinolytic protease from snake venom. Haemostasis. 1990;20(3):147-54. [PubMed:1696922]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Structural molecule activity
Specific Function
Cleaved by the protease thrombin to yield monomers which, together with fibrinogen alpha (FGA) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function...
Gene Name
FGB
Uniprot ID
P02675
Uniprot Name
Fibrinogen beta chain
Molecular Weight
55927.9 Da
References
  1. Ahmed NK, Tennant KD, Markland FS, Lacz JP: Biochemical characteristics of fibrolase, a fibrinolytic protease from snake venom. Haemostasis. 1990;20(3):147-54. [PubMed:1696922]

Drug created on October 21, 2007 16:23 / Updated on May 01, 2018 23:12