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Identification
NameOcriplasmin
Accession NumberDB08888
TypeBiotech
GroupsApproved
Description

Ocriplasmin is a recombinant truncated form of human plasmin with a molecular weight of 27.2 kDa produced by recombinant DNA technology in a Pichia pastoris expression system. Ocriplasmin is a protein made up of 249 amino acids and has two peptide chains. Agent for pharmacologic vitreolysis; thrombolytic agent. FDA approved in October 17, 2012.

Protein structureNo structure small
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Protein chemical formulaC1214H1890N338O348S14
Protein average weight27250.0 Da
Sequences
>Protein sequence for the truncated heavy chain
APSFDCGKPQVEPKKCPGR
>Protein sequence for the light chain 
VVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAH
QEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECF
ITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDS
GGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN
Download FASTA Format
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Jetreasolution2.5 mgintravitrealAlcon Canada Inc2013-11-20Not applicableCanada
Jetreasolution1.25 mgintravitrealAlcon Canada IncNot applicableNot applicableCanada
Jetreainjection, solution2.5 mg/mLintravitrealThrombo Genics Inc.2012-10-31Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7V6HE3DM5A
CAS number1048016-09-6
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationOcriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion.
PharmacodynamicsNot Available
Mechanism of actionOcriplasmin has proteolytic activity against protein components of the vitreous body and the vitreoretinal interface (VRI) (e.g. laminin, fibronectin and collagen), thereby dissolving the protein matrix responsible for the vitreomacular adhesion (VMA).
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AbsorptionBecause of the small dose administered (0.125 mg), ocriplasmin is not expected to be in the systemic circulation following injection. Within 30 minutes after injection, levels of ocriplasmin in the vitreous are 12 mcg/mL. 24 hours after injection, levels in the virtreous are 0.5 mcg/mL
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Ocriplasmin is quickly inactivated by protease inhibitor α2-antiplasmin or α2-macroglobulin.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityThe most commonly reported reactions (≥ 5%) in patients treated with ocriplasmin were vitreous floaters, conjunctival hemorrhage, eye pain, photopsia, blurred vision, macular hole, reduced visual acuity, visual impairment, and retinal edema.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solutionintravitreal2.5 mg/mL
Solutionintravitreal1.25 mg
Solutionintravitreal2.5 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesS01XA22
AHFS Codes
  • 52:92
PDB EntriesNot Available
FDA labelDownload (392 KB)
MSDSNot Available
Interactions
Drug InteractionsNo interactions found.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
cleavage
General Function:
Protease binding
Specific Function:
Fibronectins bind cell surfaces and various compounds including collagen, fibrin, heparin, DNA, and actin. Fibronectins are involved in cell adhesion, cell motility, opsonization, wound healing, and maintenance of cell shape. Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process, essential for osteoblast mineralization. Participates in t...
Gene Name:
FN1
Uniprot ID:
P02751
Molecular Weight:
262623.095 Da
References
  1. Tsui I, Pan CK, Rahimy E, Schwartz SD: Ocriplasmin for vitreoretinal diseases. J Biomed Biotechnol. 2012;2012:354979. doi: 10.1155/2012/354979. Epub 2012 Oct 14. [PubMed:23193358 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
ligand
General Function:
Tumor necrosis factor binding
Specific Function:
Is able to inhibit all four classes of proteinases by a unique 'trapping' mechanism. This protein has a peptide stretch, called the 'bait region' which contains specific cleavage sites for different proteinases. When a proteinase cleaves the bait region, a conformational change is induced in the protein which traps the proteinase. The entrapped enzyme remains active against low molecular weight...
Gene Name:
A2M
Uniprot ID:
P01023
Molecular Weight:
163289.945 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
ligand
General Function:
Serine-type endopeptidase inhibitor activity
Specific Function:
Serine protease inhibitor. The major targets of this inhibitor are plasmin and trypsin, but it also inactivates matriptase-3/TMPRSS7 and chymotrypsin.
Gene Name:
SERPINF2
Uniprot ID:
P08697
Molecular Weight:
54565.32 Da
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Drug created on May 29, 2013 00:29 / Updated on August 17, 2016 12:24