Identification

Name
Ocriplasmin
Accession Number
DB08888  (DB05028)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Recombinant Enzymes
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 chemical formula
C1214H1890N338O348S14
Protein average weight
27250.0 Da
Sequences
>Protein sequence for the truncated heavy chain
APSFDCGKPQVEPKKCPGR
>Protein sequence for the light chain 
VVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAH
QEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECF
ITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDS
GGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN
Download FASTA Format
Synonyms
  • Microplasmin
  • Microplasmin (synthetic human)
  • Ocriplasmina
  • Recombinant human microplasmin
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JetreaInjection, solution0.375 mg/0.3mlIntravitrealThrombo Genics Nv2013-03-13Not applicableEu
JetreaSolution2.5 mgIntravitrealAlcon, Inc.2013-11-20Not applicableCanada
JetreaInjection, solution1.25 mg/1mLIntravitrealThrombo Genics2017-09-18Not applicableUs
JetreaInjection, solution, concentrate0.5 mg/0.2mlIntravitrealThrombo Genics Nv2013-03-13Not applicableEu
JetreaInjection, solution2.5 mg/1mLIntravitrealThrombo Genics2012-10-312017-09-18Us
JetreaSolution1.25 mgIntravitrealAlcon, Inc.Not applicableNot applicableCanada
Categories
UNII
7V6HE3DM5A
CAS number
1048016-09-6

Pharmacology

Indication

Ocriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Ocriplasmin 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).

TargetActionsOrganism
AFibronectin
cleavage
Human
NAlpha-2-macroglobulin
ligand
Human
NAlpha-2-antiplasmin
ligand
Human
Absorption

Because 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 distribution
Not Available
Protein binding
Not Available
Metabolism

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

Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

The 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
No interactions found.
Food Interactions
Not Available

References

General References
Not Available
External Links
KEGG Drug
D09646
PubChem Substance
347910381
ChEMBL
CHEMBL2095222
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ocriplasmin
ATC Codes
S01XA22 — Ocriplasmin
FDA label
Download (392 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentCentral Retinal Vein Occlusion (CRVO)1
1, 2TerminatedTreatmentUveitis1
2Active Not RecruitingTreatmentPosterior Vitreous Detachment / Progression, Disease / Retinopathy, Diabetic1
2CompletedTreatmentDiabetic Macular Edema (DME)1
2CompletedTreatmentEye Diseases / Vitreomacular Traction Maculopathy1
2CompletedTreatmentFocal Vitreomacular Adhesion1
2CompletedTreatmentFocal Vitreomacular Adhesion / Neovascular Age-Related Macular Degeneration1
2CompletedTreatmentStroke, Acute1
2CompletedTreatmentVitrectomy therapy3
2CompletedTreatmentVitreomacular Traction1
2TerminatedTreatmentArterial Occlusive Diseases1
2TerminatedTreatmentDeep Vein Thrombosis (DVT)1
2TerminatedTreatmentStrokes1
2Unknown StatusTreatmentMacular Degeneration1
3CompletedTreatmentSymptomatic Vitreomacular Adhesion1
3CompletedTreatmentVitreomacular Adhesion2
3CompletedTreatmentVitreomacular Adhesion Including Macular Hole1
4CompletedTreatmentVitreomacular Adhesion / Vitreomacular Traction2
Not AvailableCompletedNot AvailableSymptomatic Vitreomacular Adhesion1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionIntravitreal0.375 mg/0.3ml
Injection, solutionIntravitreal1.25 mg/1mL
Injection, solutionIntravitreal2.5 mg/1mL
Injection, solution, concentrateIntravitreal0.5 mg/0.2ml
SolutionIntravitreal1.25 mg
SolutionIntravitreal2.5 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

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

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, an...
Gene Name
FN1
Uniprot ID
P02751
Uniprot Name
Fibronectin
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 differen...
Gene Name
A2M
Uniprot ID
P01023
Uniprot Name
Alpha-2-macroglobulin
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
Uniprot Name
Alpha-2-antiplasmin
Molecular Weight
54565.32 Da

Drug created on May 29, 2013 00:29 / Updated on November 05, 2018 17:49