| Primary information |
|---|
| ThPP ID | Th1095 |
| Therapeutic Peptide/Protein Name | Ranibizumab |
| Sequence | Raibizumab Light Chain SASQDISNYLNWYQQKPGKAPKVLIYF view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 48349.611 |
| Chemical Formula | C2158H3282N562O681S12 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | Approximately 9 days. |
| Description | Recombinant (E.coli derived), humanized IgG1 kappa isotype monoclonal antibody (intraocular use). It binds to and inhibits the biologic activity of human vascular endothelial growth factor A (VEGF-A). Ranibizumab is marketed under the name Lucentis. |
| Indication/Disease | For the treatment of patients with macular edema after retinal vein occlusion, age-related macular degeneration (wet), and diabetic macular edema. |
| Pharmacodynamics | Ranibizumab is a recombinant humanized IgG1 kappa isotype monoclonal antibody fragment designed for intraocular use. Ranibizumab is a VEGF-A antagonist that binds to and inhibits the biologic activity of active forms of human VEGF-A, including the cleaved form (VEGF110). VEGF-A has been shown to cause neovascularization (angiogenesis) and an increase in vascular permeability, which is thought to contribute to the progression of the neovascular form of age-related macular degeneration (AMD). |
| Mechanism of Action | Ranibizumab binds to the receptor binding site of active forms of VEGF-A, including the biologically active, cleaved form of this molecule, (VEGF110). The binding of ranibizumab to VEGF-A prevents the interaction of VEGF-A with its receptors (VEGFR1 and VEGFR2) on the surface of endothelial cells, reducing endothelial cell proliferation, vascular leakage, and new blood vessel formation. |
| Toxicity | The most common toxic effects to the eye are eye pain, vitreous floaters, increased intraocular pressure, conjunctival hemorrhage, intraocular inflammation, and foreign body sensation. Also arterial thromboembolic events have occurred in patients. |
| Metabolism | Metabolism was not quantified. |
| Absorption | After monthly intravitreal injections, maximum serum concentrations are minimal around 0.3 ng/mL to 2.36 ng/mL. |
| Volume of Distribution | Volume of distribution is insignificant. |
| Clearance | Clearance was not quantified. |
| Categories | Ophthalmics |
| Patents Number | CA2286330 |
| Date of Issue | 11/06/12 |
| Date of Expiry | 04/04/22 |
| Drug Interaction | N.A. |
| Target | Vascular endothelial growth factor A |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Lucentis |
| Company | Genentech |
| Brand Discription | LUCENTIS(ranibizumab injection) is a recombinant humanized IgG1 kappa isotype monoclonal antibody fragment designed for intraocular use. Ranibizumab binds to and inhibits the biologic activity of human vascular endothelial growth factor A (VEGF-A). Ranibizumab, which lacks an Fc region, has a molecular weight of approximately 48 kilodaltons and is produced by an E. coli expression system in a nutrient medium containing the antibiotic tetracycline. Tetracycline is not detectable in the final product. |
| Prescribed for | Neovascular (Wet) Age-Related Macular Degeneration (AMD), Macular Edema Following Retinal Vein Occlusion (RVO), Diabetic Macular Edema (DME), Diabetic Retinopathy (Non Proliferative Diabetic Retinopathy (NPDR), Proliferative Diabetic Retinopathy (PDR)) In patients With Diabetic Macular Edema (DME) |
| Chemical Name | N.A. |
| Formulation | supplied as a preservative-free, sterile solution in a single-use glass vial designed to deliver 0.05 mL of 10 mg/mL LUCENTIS (0.5 mg dose vial) or 6 mg/mL LUCENTIS (0.3 mg dose vial) aqueous solution with 10 mM histidine HCl, 10% α,α-trehalose dihydrate, 0.01% polysorbate 20, pH 5.5. |
| Physcial Appearnce | Sterile, colorless to pale yellow solution in a single-use glass vial |
| Route of Administration | Intravitreal Injection ONLY |
| Recommended Dosage | Neovascular (Wet) Age-Related Macular Degeneration (AMD): LUCENTIS 0.5 mg (0.05 mL of 10 mg/mL LUCENTIS solution) is recommended to be administered by intravitreal injection once a month (approximately 28 days). LUCENTIS 0.5 mg (0.05 mL of 10 mg/mL LUCENTIS solution) is recommended to be administered by intravitreal injection once a month (approximately 28 days). Diabetic Macular Edema (DME): LUCENTIS 0.3 mg (0.05 mL of 6 mg/mL LUCENTIS solution) is recommended to be administered by intravitreal injection once a month (approximately 28 days).; Diabetic Retinopathy In Patients With Diabetic Macular Edema: LUCENTIS 0.3 mg (0.05 mL of 6 mg/mL LUCENTIS solution) is recommended to be administered by intravitreal injection once a month (approximately 28 days). |
| Contraindication | Ocular Or Periocular Infections LUCENTIS is contraindicated in patients with ocular or periocular infections. Hypersensitivity to ranibizumab or any of the excipients in LUCENTIS. Hypersensitivity reactions may manifest as severe intraocular inflammation. |
| Side Effects | Endophthalmitis and Retinal Detachments Increases in Intraocular Pressure, Thromboembolic Events, Fatal Events in patients with DME and DR at baseline. |
| Useful Link | http://www.rxlist.com/lucentis-drug/side-effects-interactions.htm http://www.fda.gov/Safety/MedWatch/SafetyInformation/ucm316365.htm http://www.gene.com/media/product-information/lucentis |
| PubMed ID | 25631483, 25627091, 18054637, 18046235, 18035187, 15671306, 17687925, 25646034, 23560774 |
| 3-D Structure | N.A. |