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10650 details
Primary information
ID10650
Therapeutic IDTh1135
Protein NameOcriplasmin
Sequence>Th1135_Ocriplasmin APSFDCGKPQVEPKKCPGR
Molecular Weight27250
Chemical FormulaC1214H1890N338O348S14
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeNA
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.
PharmacodynamicsNA
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 a2-antiplasmin or a2-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
NA
ClearanceNA
CategoriesOphthalmics
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetFibronectin,Alpha-2-macroglobulin,Alpha-2-antiplasmin
Brand NameJetrea
CompanyThromboGenics NV
Brand DescriptionThromboGenics NV
Prescribed Forsymptomatic vitreomacular adhesion.
Chemical NameNA
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.
Physical Appearance JETREA is a Sterile, clear and colorless solution with no preservatives
Route of AdministrationIntravitreal Injection
Recommended Dosage0.125 mg (0.1 mL of the diluted solution)
ContraindicationNA
Side EffectsDecreased Vision, Intravitreal Injection Procedure Associated Effects, Potential for Lens Subluxation, Retinal Breaks
Useful Link 1Link
Useful Link 2NA
RemarksNA