Egaptivon pegol

Identification

Generic Name
Egaptivon pegol
DrugBank Accession Number
DB05202
Background

ARC1779 is a therapeutic aptamer antagonist of the A1 domain of von Willebrand Factor (vWF), the ligand for receptor glycoprotein 1b on platelets. ARC1779 is being developed as a novel antithrombotic agent for use in patients with acute coronary syndromes. ARC1779 is a therapeutic oligonucleotide ("aptamer") which blocks the binding of the A1 domain of vWF to the platelet GPIb receptor, and thereby modulates platelet adhesion, activation, and aggregation under the high shear conditions of coronary arterial stenosis and plaque rupture.

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
  • Egaptivon pegol
External IDs
  • ARC1779

Pharmacology

Indication

Platelet aggregation, thrombosis and acute coronary syndromes

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Pharmacodynamics

Not Available

Mechanism of action

ARC1779 can inhibit vWF activation and platelet function, which are both widely recognized as playing critical roles in clot formation which can critically impede blood flow to the heart.

TargetActionsOrganism
Uvon Willebrand factorNot AvailableHumans
UPlatelet glycoprotein Ib alpha chainNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

ARC1779 was shown to bind specifically to activated vWF. Activated vWF is scientifically recognized as the first stage of arterial thrombus formation and plays a significant role in the development of harmful blood clots.

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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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.
DrugInteraction
Antihemophilic factor (recombinant), PEGylatedThe therapeutic efficacy of Antihemophilic factor (recombinant), PEGylated can be decreased when used in combination with Egaptivon pegol.
Certolizumab pegolThe therapeutic efficacy of Certolizumab pegol can be decreased when used in combination with Egaptivon pegol.
Damoctocog alfa pegolThe therapeutic efficacy of Damoctocog alfa pegol can be decreased when used in combination with Egaptivon pegol.
ElapegademaseThe therapeutic efficacy of Elapegademase can be decreased when used in combination with Egaptivon pegol.
LipegfilgrastimThe therapeutic efficacy of Lipegfilgrastim can be decreased when used in combination with Egaptivon pegol.
Methoxy polyethylene glycol-epoetin betaThe therapeutic efficacy of Methoxy polyethylene glycol-epoetin beta can be decreased when used in combination with Egaptivon pegol.
Nonacog beta pegolThe therapeutic efficacy of Nonacog beta pegol can be decreased when used in combination with Egaptivon pegol.
PegademaseThe therapeutic efficacy of Egaptivon pegol can be decreased when used in combination with Pegademase.
PegaptanibThe therapeutic efficacy of Egaptivon pegol can be decreased when used in combination with Pegaptanib.
PegaspargaseThe therapeutic efficacy of Egaptivon pegol can be decreased when used in combination with Pegaspargase.
Interactions
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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
Not Available

Chemical Identifiers

UNII
DT0445S65M
CAS number
934868-74-3

References

General References
  1. Gilbert JC, DeFeo-Fraulini T, Hutabarat RM, Horvath CJ, Merlino PG, Marsh HN, Healy JM, Boufakhreddine S, Holohan TV, Schaub RG: First-in-human evaluation of anti von Willebrand factor therapeutic aptamer ARC1779 in healthy volunteers. Circulation. 2007 Dec 4;116(23):2678-86. Epub 2007 Nov 19. [Article]
PubChem Substance
347910022

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentThrombotic Thrombocytopenic Purpura (TTP) / Von Willebrand Disease Type-2b1
2TerminatedTreatmentCerebral Thromboembolism / Intracranial Embolism / Stenosis, Carotid1
2TerminatedTreatmentThrombotic Microangiopathies / Thrombotic Thrombocytopenic Purpura (TTP)1
2WithdrawnTreatmentVon Willebrand's Disease1
1CompletedTreatmentThrombotic events1

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

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein n-terminus binding
Specific Function
Important in the maintenance of hemostasis, it promotes adhesion of platelets to the sites of vascular injury by forming a molecular bridge between sub-endothelial collagen matrix and platelet-surf...
Gene Name
VWF
Uniprot ID
P04275
Uniprot Name
von Willebrand factor
Molecular Weight
309261.83 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Thrombin receptor activity
Specific Function
GP-Ib, a surface membrane protein of platelets, participates in the formation of platelet plugs by binding to the A1 domain of vWF, which is already bound to the subendothelium.
Gene Name
GP1BA
Uniprot ID
P07359
Uniprot Name
Platelet glycoprotein Ib alpha chain
Molecular Weight
71539.265 Da

Drug created on October 21, 2007 22:24 / Updated on February 21, 2021 18:51