NAV

Alfimeprase

Identification

Generic Name
Alfimeprase
DrugBank Accession Number
DB04919
Background

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.

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
>Alfimeprase Sequence
SFPQRYVQLVIVADHRMNTKYNGDSDKIRQWVHQIVNTINEIYRPLNIQFTLVGLEIWSN
QDLITVTSVSHDTLASFGNWRETDLLRRQRHDNAQLLTAIDFDGDTVGLAYVGGMCQLKH
STGVIQDHSAINLLVALTMAHELGHNLGMNHDGNQCHCGANSCVMAAMLSDQPSKLFSDC
SKKDYQTFLTVNNPQCILNKP
Download FASTA Format
Synonyms
  • 3-203-FIBROLASE (3-SERINE) (AGKISTRODON CONTORTRIX CONTORTRIX RECOMBINANT)
  • Alfimeprase
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Pharmacology

Indication

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

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Contraindications & Blackbox Warnings
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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 AvailableHumans
UFibrinogen beta chainNot AvailableHumans
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

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
GPN9HBH1HS
CAS number
259074-76-5

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. [Article]
PubChem Substance
347909847

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentArterial Occlusive Diseases1
3CompletedTreatmentCatheter Occlusion / Thrombosis / Venous Thrombosis (Disorder)1
3CompletedTreatmentThrombosis / Venous Thrombosis (Disorder)1
3TerminatedTreatmentArterial Occlusive Diseases1
2CompletedTreatmentArterial Occlusive Diseases / Peripheral Vascular Disease Patient / Thrombosis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

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Details1. Fibrinogen alpha chain
Kind
Protein
Organism
Humans
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. [Article]
Details2. Fibrinogen beta chain
Kind
Protein
Organism
Humans
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. [Article]

Drug created at October 21, 2007 22:23 / Updated at September 30, 2023 19:51