==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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1622 details
Primary information
ThPP IDTh1135
Therapeutic Peptide/Protein NameOcriplasmin
SequenceTruncated heavy chain: APSFDCGKPQVEPKKCPGR Light c view full sequnce in fasta
Functional ClassificationIc
Molecular Weight272500
Chemical FormulaC1214H1890N338O348S14
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeN.A.
DescriptionOcriplasmin is a recombinant (derived from Pichia pastoris) truncated form of human plasmin with a molecular weight of 27.2 kDa. It is a 249 amino acid protein that is made up of two peptide chains. Agent for pharmacologic vitreolysis; thrombolytic agent. FDA approved on October 17, 2012.
Indication/DiseaseOcriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion.
PharmacodynamicsN.A.
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).
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.
MetabolismOcriplasmin is quickly inactivated by protease inhibitor α2-antiplasmin or α2-macroglobulin.
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 DistributionN.A.
ClearanceN.A.
CategoriesOphthalmics
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetFibronectin,Alpha-2-macroglobulin,Alpha-2-antiplasmin
Information of corresponding available drug in the market
Brand NameJetrea
CompanyThromboGenics NV
Brand DiscriptionOcriplasmin 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.
Prescribed forsymptomatic vitreomacular adhesion.
Chemical NameN.A.
FormulationEach vial contains 0.5 mg ocriplasmin (active) and 0.21 mg citric acid, 0.75 mg mannitol, sodium hydroxide (for pH adjustment) and water for injection. The pH of the solution is 3.1.
Physcial AppearnceJETREA is a Sterile, clear and colorless solution with no preservatives
Route of AdministrationIntravitreal Injection
Recommended Dosage 0.125 mg (0.1 mL of the diluted solution)
ContraindicationN.A.
Side EffectsDecreased Vision, Intravitreal Injection Procedure Associated Effects, Potential for Lens Subluxation, Retinal Breaks
Useful Linkhttp://www.rxlist.com/jetrea-drug.htm http://jetrea.com/ http://www.drugs.com/history/jetrea.html
PubMed ID25635577, 25635575, 25606039, 25582211, 25580329
3-D StructureTh1135 Heavy chianor (Download), Th1135 Light chian (View) or (Download)