Ocriplasmin
Explore a selection of our essential drug information below, or:
Identification
- Summary
Ocriplasmin is a proteolytic enzyme used to treat symptomatic vitreomacular adhesion by dissolving the protein matrix responsible for the adhesion between the vitreous and macula.
- Generic Name
- Ocriplasmin
- DrugBank Accession Number
- DB08888
- Background
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.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Recombinant Enzymes - 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)
- Ocriplasmin
- Ocriplasmina
- Recombinant human microplasmin
Pharmacology
- Indication
Ocriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Symptomatic vitreomacular adhesion •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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).
Target Actions Organism AFibronectin cleavageHumans NAlpha-2-macroglobulin ligandHumans NAlpha-2-antiplasmin ligandHumans - 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
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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.
- 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.No interactions found.
- Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Jetrea Solution 1.25 mg / mL Intravitreal Thrombogenics Nv 2019-05-08 2020-03-20 Canada Jetrea Injection, solution 2.5 mg/1mL Intravitreal Thrombo Genics 2012-10-31 2017-09-18 US Jetrea Injection, solution 0.375 mg/0.3ml Intravitreal Inceptua Ab 2016-09-08 2013-01-17 EU Jetrea Solution 2.5 mg / mL Intravitreal Thrombogenics Nv 2013-11-20 2020-03-10 Canada Jetrea Injection, solution, concentrate 0.5 mg/0.2ml Intravitreal Inceptua Ab 2016-09-08 2013-01-17 EU
Categories
- ATC Codes
- S01XA22 — Ocriplasmin
- 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
- 7V6HE3DM5A
- CAS number
- 1048016-09-6
References
- General References
- Not Available
- External Links
- KEGG Drug
- D09646
- PubChem Substance
- 347910381
- 29998
- ChEMBL
- CHEMBL2095222
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ocriplasmin
- FDA label
- Download (392 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Symptomatic Vitreomacular Adhesion (VMA) 1 somestatus stop reason just information to hide 4 Completed Treatment Vitreomacular Adhesion / Vitreomacular Traction (VMT) 2 somestatus stop reason just information to hide 3 Completed Treatment Symptomatic Vitreomacular Adhesion (VMA) 1 somestatus stop reason just information to hide 3 Completed Treatment Vitreomacular Adhesion 2 somestatus stop reason just information to hide 3 Completed Treatment Vitreomacular Adhesion Including Macular Hole 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravitreal 0.375 MG/0.3ML Injection, solution Intravitreal 1.25 mg/1mL Injection, solution Intravitreal 2.5 mg/1mL Injection, solution, concentrate Intravitreal 0.5 mg/0.2ml Solution Intravitreal 1.25 mg / mL Solution Intravitreal 2.5 mg / mL Solution, concentrate Intravitreal 0.5 MG/0.2ML - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Cleavage
- General Function
- Fibronectins bind cell surfaces and various compounds including collagen, fibrin, heparin, DNA, and actin (PubMed:3024962, PubMed:3593230, PubMed:3900070, PubMed:7989369). Fibronectins are involved in cell adhesion, cell motility, opsonization, wound healing, and maintenance of cell shape (PubMed:3024962, PubMed:3593230, PubMed:3900070, PubMed:7989369). Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process, essential for osteoblast mineralization (By similarity). Participates in the regulation of type I collagen deposition by osteoblasts (By similarity). Acts as a ligand for the LILRB4 receptor, inhibiting FCGR1A/CD64-mediated monocyte activation (PubMed:34089617)
- Specific Function
- collagen binding
- Gene Name
- FN1
- Uniprot ID
- P02751
- Uniprot Name
- Fibronectin
- Molecular Weight
- 272318.79 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Ligand
- General 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 substrates (activity against high molecular weight substrates is greatly reduced). Following cleavage in the bait region, a thioester bond is hydrolyzed and mediates the covalent binding of the protein to the proteinase
- Specific Function
- brain-derived neurotrophic factor binding
- Gene Name
- A2M
- Uniprot ID
- P01023
- Uniprot Name
- Alpha-2-macroglobulin
- Molecular Weight
- 163289.945 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Ligand
- General Function
- Serine protease inhibitor. The major targets of this inhibitor are plasmin and trypsin, but it also inactivates matriptase-3/TMPRSS7 and chymotrypsin
- Specific Function
- endopeptidase inhibitor activity
- Gene Name
- SERPINF2
- Uniprot ID
- P08697
- Uniprot Name
- Alpha-2-antiplasmin
- Molecular Weight
- 54565.32 Da
Drug created at May 29, 2013 06:29 / Updated at October 21, 2024 08:50