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Th1095 details

Primary information
ID 1475
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% Î±,Î±-trehalose dihydrate, 0.01% polysorbate 20, pH 5.5.
Physcial Appearance 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.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1475
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% Î±,Î±-trehalose dihydrate, 0.01% polysorbate 20, pH 5.5.
Physcial Appearance	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.