| Primary information |
|---|
| ID | 1622 |
| ThPP ID | Th1135 |
| Therapeutic Peptide/Protein Name | Ocriplasmin |
| Sequence | Truncated heavy chain: APSFDCGKPQVEPKKCPGR Light c view full sequnce in fasta |
| Functional Classification | Ic |
| Molecular Weight | 272500 |
| Chemical Formula | C1214H1890N338O348S14 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Ocriplasmin 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/Disease | Ocriplasmin is a proteolytic enzyme indicated for the treatment for symptomatic vitreomacular adhesion. |
| Pharmacodynamics | N.A. |
| 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). |
| 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. |
| Metabolism | Ocriplasmin is quickly inactivated by protease inhibitor α2-antiplasmin or α2-macroglobulin. |
| 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 | N.A. |
| Clearance | N.A. |
| Categories | Ophthalmics |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Fibronectin,Alpha-2-macroglobulin,Alpha-2-antiplasmin |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Jetrea |
| Company | ThromboGenics NV |
| Brand Discription | 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. |
| Prescribed for | symptomatic vitreomacular adhesion. |
| Chemical Name | N.A. |
| Formulation | Each 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 Appearance | JETREA is a Sterile, clear and colorless solution with no preservatives |
| Route of Administration | Intravitreal Injection |
| Recommended Dosage | 0.125 mg (0.1 mL of the diluted solution) |
| Contraindication | N.A. |
| Side Effects | Decreased Vision, Intravitreal Injection Procedure Associated Effects, Potential for Lens Subluxation, Retinal Breaks |
| Useful Link | http://www.rxlist.com/jetrea-drug.htm http://jetrea.com/ http://www.drugs.com/history/jetrea.html |
| PubMed ID | 25635577, 25635575, 25606039, 25582211, 25580329 |
| 3-D Structure | Th1135 Heavy chianor (Download), Th1135 Light chian (View) or (Download) |