Explore a selection of our essential drug information below, or:
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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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.
Target Actions Organism UFibrinogen alpha chain Not Available Humans - 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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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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- External Links
- PubChem Substance
- 347910189
Clinical Trials
- Clinical Trials
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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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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General 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 in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways
- Specific Function
- Extracellular matrix structural constituent
- Gene Name
- FGA
- Uniprot ID
- P02671
- Uniprot Name
- Fibrinogen alpha chain
- Molecular Weight
- 94972.455 Da
References
- 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]
- 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