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Identification
NameRanibizumab
Accession NumberDB01270
TypeBiotech
GroupsApproved
Description

Ranibizumab 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 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). Ranibizumab is marketed under the name Lucentis®. It is indicated for the treatment of macular edema after retinal vein occlusion, age-related macular degeneration (wet), and diabetic macular edema.

Protein structureDb01270
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Protein chemical formulaC2158H3282N562O681S12
Protein average weight48349.611 Da
Sequences
>Ranibizumab Light Chain
DIQLTQSPSSLSASVGDRVTITCSASQDISNYLNWYQQKPGKAPKVLIYFTSSLHSGVPS
RFSGSGSGTDFTLTISSLQPEDFATYYCQQYSTVPWTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Ranibizumab Heavy Chain
EVQLVESGGGLVQPGGSLRLSCAASGYDFTHYGMNWVRQAPGKGLEWVGWINTYTGEPTY
AADFKRRFTFSLDTSKSTAYLQMNSLRAEDTAVYYCAKYPYYYGTSHWYFDVWGQGTLVT
VSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVL
QSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHL
Download FASTA Format
Synonyms
rhuFab V2
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Lucentisinjection, solution10 mg/mLintravitrealGenentech, Inc.2006-06-30Not applicableUs
Lucentissolution10 mgintravitrealNovartis Pharmaceuticals Canada Inc2014-09-18Not applicableCanada
Lucentissolution10 mgintravitrealNovartis Pharmaceuticals Canada Inc2007-07-26Not applicableCanada
Lucentisinjection, solution6 mg/mLintravitrealGenentech, Inc.2012-08-10Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIZL1R02VT79
CAS number347396-82-1
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of patients with macular edema after retinal vein occlusion, age-related macular degeneration (wet), and diabetic macular edema.
PharmacodynamicsRanibizumab 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 actionRanibizumab 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.
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AbsorptionAfter 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.

Protein bindingPlasma protein binding is insignificant.
Metabolism

Metabolism was not quantified.

Route of eliminationNot Available
Half lifeApproximately 9 days.
Clearance

Clearance was not quantified.

ToxicityThe 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.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravitreal10 mg/mL
Injection, solutionintravitreal6 mg/mL
Solutionintravitreal10 mg
Prices
Unit descriptionCostUnit
Lucentis 0.5 mg vial2340.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2286330 No2008-06-102018-04-03Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting pointNot applicableFrom MSDS.
boiling pointApproximately 100 degrees CFrom MSDS.
water solubilitySoluble in water.From MSDS.
References
Synthesis ReferenceNot Available
General References
  1. Gaudreault J, Fei D, Beyer JC, Ryan A, Rangell L, Shiu V, Damico LA: Pharmacokinetics and retinal distribution of ranibizumab, a humanized antibody fragment directed against VEGF-A, following intravitreal administration in rabbits. Retina. 2007 Nov-Dec;27(9):1260-6. [PubMed:18046235 ]
  2. Gaudreault J, Fei D, Rusit J, Suboc P, Shiu V: Preclinical pharmacokinetics of Ranibizumab (rhuFabV2) after a single intravitreal administration. Invest Ophthalmol Vis Sci. 2005 Feb;46(2):726-33. [PubMed:15671306 ]
  3. Bakri SJ, Snyder MR, Reid JM, Pulido JS, Ezzat MK, Singh RJ: Pharmacokinetics of intravitreal ranibizumab (Lucentis). Ophthalmology. 2007 Dec;114(12):2179-82. [PubMed:18054637 ]
  4. Kourlas H, Abrams P: Ranibizumab for the treatment of neovascular age-related macular degeneration: a review. Clin Ther. 2007 Sep;29(9):1850-61. [PubMed:18035187 ]
External Links
ATC CodesS01LA04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (383 KB)
MSDSDownload (95.8 KB)
Interactions
Drug Interactions
Drug
BelimumabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Belimumab.
Food Interactions
  • No food effects found.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Vascular endothelial growth factor receptor binding
Specific Function:
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activ...
Gene Name:
VEGFA
Uniprot ID:
P15692
Molecular Weight:
27042.205 Da
References
  1. Gaudreault J, Fei D, Rusit J, Suboc P, Shiu V: Preclinical pharmacokinetics of Ranibizumab (rhuFabV2) after a single intravitreal administration. Invest Ophthalmol Vis Sci. 2005 Feb;46(2):726-33. [PubMed:15671306 ]
  2. Michels S, Rosenfeld PJ: [Treatment of neovascular age-related macular degeneration with Ranibizumab/Lucentis]. Klin Monbl Augenheilkd. 2005 Jun;222(6):480-4. [PubMed:15973626 ]
  3. Rosenfeld PJ, Rich RM, Lalwani GA: Ranibizumab: Phase III clinical trial results. Ophthalmol Clin North Am. 2006 Sep;19(3):361-72. [PubMed:16935211 ]
  4. Nguyen QD, Tatlipinar S, Shah SM, Haller JA, Quinlan E, Sung J, Zimmer-Galler I, Do DV, Campochiaro PA: Vascular endothelial growth factor is a critical stimulus for diabetic macular edema. Am J Ophthalmol. 2006 Dec;142(6):961-9. Epub 2006 Aug 2. [PubMed:17046701 ]
  5. Pieramici DJ, Avery RL: Ranibizumab: treatment in patients with neovascular age-related macular degeneration. Expert Opin Biol Ther. 2006 Nov;6(11):1237-45. [PubMed:17049020 ]
  6. Gaudreault J, Fei D, Beyer JC, Ryan A, Rangell L, Shiu V, Damico LA: Pharmacokinetics and retinal distribution of ranibizumab, a humanized antibody fragment directed against VEGF-A, following intravitreal administration in rabbits. Retina. 2007 Nov-Dec;27(9):1260-6. [PubMed:18046235 ]
  7. Ferrara N, Damico L, Shams N, Lowman H, Kim R: Development of ranibizumab, an anti-vascular endothelial growth factor antigen binding fragment, as therapy for neovascular age-related macular degeneration. Retina. 2006 Oct;26(8):859-70. [PubMed:17031284 ]
  8. Bakri SJ, Snyder MR, Reid JM, Pulido JS, Ezzat MK, Singh RJ: Pharmacokinetics of intravitreal ranibizumab (Lucentis). Ophthalmology. 2007 Dec;114(12):2179-82. [PubMed:18054637 ]
  9. Kourlas H, Abrams P: Ranibizumab for the treatment of neovascular age-related macular degeneration: a review. Clin Ther. 2007 Sep;29(9):1850-61. [PubMed:18035187 ]
  10. Spitzer MS, Ziemssen F, Bartz-Schmidt KU, Gelisken F, Szurman P: Treatment of age-related macular degeneration: focus on ranibizumab. Clin Ophthalmol. 2008 Mar;2(1):1-14. [PubMed:19668384 ]
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Drug created on May 16, 2007 14:14 / Updated on March 14, 2016 09:59