NAV

EP-2104R

Identification

Generic Name
EP-2104R
DrugBank Accession Number
DB05675
Background

EP-2104R is an imaging pharmaceutical under development for the detection of blood clots. It is the first targeted high-resolution technique designed to visualize blood clots directly. It is being developed by EPIX Pharmaceuticals, Inc.

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
Not Available
External IDs
  • EP 2104R
  • EP-2104R

Pharmacology

Indication

Investigated for use/treatment in cardiovascular disorders and thrombosis.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

EP-2104R is a gadolinium-based small peptide with high affinity and specificity for human fibrin. Molecular MR imaging with the fibrin-targeted contrast-agent EP-2104R allows selective visualization of acute coronary, cardiac, and pulmonary thrombi.

Mechanism of action

EP-2104R binds specifically to fibrin, a protein present in all blood clots. When bound, it can be detected using a magnetic resonance imaging (MRI) scan.

TargetActionsOrganism
UFibrinogen alpha 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
Not Available
CAS number
Not Available

References

General References
  1. Botnar RM, Buecker A, Wiethoff AJ, Parsons EC Jr, Katoh M, Katsimaglis G, Weisskoff RM, Lauffer RB, Graham PB, Gunther RW, Manning WJ, Spuentrup E: In vivo magnetic resonance imaging of coronary thrombosis using a fibrin-binding molecular magnetic resonance contrast agent. Circulation. 2004 Sep 14;110(11):1463-6. Epub 2004 Jul 6. [Article]
  2. Spuentrup E, Buecker A, Katoh M, Wiethoff AJ, Parsons EC Jr, Botnar RM, Weisskoff RM, Graham PB, Manning WJ, Gunther RW: Molecular magnetic resonance imaging of coronary thrombosis and pulmonary emboli with a novel fibrin-targeted contrast agent. Circulation. 2005 Mar 22;111(11):1377-82. Epub 2005 Feb 28. [Article]
  3. Spuentrup E, Katoh M, Wiethoff AJ, Parsons EC Jr, Botnar RM, Mahnken AH, Gunther RW, Buecker A: Molecular magnetic resonance imaging of pulmonary emboli with a fibrin-specific contrast agent. Am J Respir Crit Care Med. 2005 Aug 15;172(4):494-500. Epub 2005 Jun 3. [Article]
  4. Spuentrup E, Fausten B, Kinzel S, Wiethoff AJ, Botnar RM, Graham PB, Haller S, Katoh M, Parsons EC Jr, Manning WJ, Busch T, Gunther RW, Buecker A: Molecular magnetic resonance imaging of atrial clots in a swine model. Circulation. 2005 Jul 19;112(3):396-9. Epub 2005 Jul 11. [Article]
  5. Sirol M, Fuster V, Badimon JJ, Fallon JT, Moreno PR, Toussaint JF, Fayad ZA: Chronic thrombus detection with in vivo magnetic resonance imaging and a fibrin-targeted contrast agent. Circulation. 2005 Sep 13;112(11):1594-600. Epub 2005 Sep 6. [Article]
  6. Stracke CP, Katoh M, Wiethoff AJ, Parsons EC, Spangenberg P, Spuntrup E: Molecular MRI of cerebral venous sinus thrombosis using a new fibrin-specific MR contrast agent. Stroke. 2007 May;38(5):1476-81. Epub 2007 Mar 22. [Article]
  7. Spuentrup E, Katoh M, Buecker A, Fausten B, Wiethoff AJ, Wildberger JE, Haage P, Parsons EC Jr, Botnar RM, Graham PB, Vettelschoss M, Gunther RW: Molecular MR imaging of human thrombi in a swine model of pulmonary embolism using a fibrin-specific contrast agent. Invest Radiol. 2007 Aug;42(8):586-95. [Article]
  8. Spuentrup E, Katoh M, Wiethoff AJ, Buecker A, Botnar RM, Parsons EC, Guenther RW: Molecular coronary MR imaging of human thrombi using EP-2104R, a fibrin-targeted contrast agent: experimental study in a swine model. Rofo. 2007 Nov;179(11):1166-73. [Article]
  9. Vymazal J, Spuentrup E, Cardenas-Molina G, Wiethoff AJ, Hartmann MG, Caravan P, Parsons EC Jr: Thrombus imaging with fibrin-specific gadolinium-based MR contrast agent EP-2104R: results of a phase II clinical study of feasibility. Invest Radiol. 2009 Nov;44(11):697-704. doi: 10.1097/RLI.0b013e3181b092a7. [Article]
PubChem Substance
347910189

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

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

Properties

State
Solid
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. Spuentrup E, Katoh M, Buecker A, Fausten B, Wiethoff AJ, Wildberger JE, Haage P, Parsons EC Jr, Botnar RM, Graham PB, Vettelschoss M, Gunther RW: Molecular MR imaging of human thrombi in a swine model of pulmonary embolism using a fibrin-specific contrast agent. Invest Radiol. 2007 Aug;42(8):586-95. [Article]
  2. Spuentrup E, Katoh M, Wiethoff AJ, Buecker A, Botnar RM, Parsons EC, Guenther RW: Molecular coronary MR imaging of human thrombi using EP-2104R, a fibrin-targeted contrast agent: experimental study in a swine model. Rofo. 2007 Nov;179(11):1166-73. [Article]

Drug created at November 18, 2007 18:26 / Updated at June 12, 2020 16:52