Ranibizumab

Identification

Summary

Ranibizumab is a recombinant humanized monoclonal antibody and VEGF-A antagonist used for the management of macular edema after retinal vein occlusion, age-related macular degeneration (wet), and diabetic macular edema.

Brand Names
Lucentis
Generic Name
Ranibizumab
DrugBank Accession Number
DB01270
Background

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.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db01270
Protein Chemical Formula
C2158H3282N562O681S12
Protein Average Weight
48349.611 Da
Sequences
>Ranibizumab Light Chain
DIQLTQSPSSLSASVGDRVTITCSASQDISNYLNWYQQKPGKAPKVLIYFTSSLHSGVPS
RFSGSGSGTDFTLTISSLQPEDFATYYCQQYSTVPWTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Ranibizumab Heavy Chain
EVQLVESGGGLVQPGGSLRLSCAASGYDFTHYGMNWVRQAPGKGLEWVGWINTYTGEPTY
AADFKRRFTFSLDTSKSTAYLQMNSLRAEDTAVYYCAKYPYYYGTSHWYFDVWGQGTLVT
VSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVL
QSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHL
Download FASTA Format
Synonyms
  • Ranibizumab
  • rhuFab V2
External IDs
  • RG-3645

Pharmacology

Indication

For the treatment of patients with macular edema after retinal vein occlusion, age-related macular degeneration (wet), and diabetic macular edema.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
AVascular endothelial growth factor ANot AvailableHumans
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.

Protein binding

Plasma protein binding is insignificant.

Metabolism

Metabolism was not quantified.

Route of elimination

Not Available

Half-life

Approximately 9 days.

Clearance

Clearance was not quantified.

Adverse Effects
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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.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Ranibizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Ranibizumab.
AducanumabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Aducanumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ranibizumab.
Alendronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Ranibizumab is combined with Alendronic acid.
AlirocumabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Alirocumab.
AmivantamabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Amivantamab.
AnsuvimabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Ansuvimab.
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Anthrax immune globulin human.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Ranibizumab is combined with Antilymphocyte immunoglobulin (horse).
Interactions
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Food Interactions
  • Take with or without food.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LucentisInjection, solution6 mg/1mLIntravitrealGenentech, Inc.2012-08-10Not applicableUS flag
LucentisSolution10 mg / mLIntravitrealNovartis2007-07-26Not applicableCanada flag
LucentisInjection, solution10 mg/mlIntravitrealNovartis Europharm Limited2016-09-08Not applicableEU flag
LucentisInjection, solution10 mg/mlIntravitrealNovartis Europharm Limited2016-09-08Not applicableEU flag
LucentisInjection, solution10 mg/1mLIntravitrealGenentech, Inc.2006-06-30Not applicableUS flag
LucentisInjection, solution10 mg/mlIntravitrealNovartis Europharm Limited2016-09-08Not applicableEU flag
LucentisSolution10 mg / mLIntravitrealNovartis2014-09-18Not applicableCanada flag
LucentisInjection, solution10 mg/mlIntravitrealNovartis Europharm Limited2016-09-08Not applicableEU flag

Categories

ATC Codes
S01LA04 — Ranibizumab
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
ZL1R02VT79
CAS number
347396-82-1

References

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
KEGG Drug
D05697
PubChem Substance
46506960
RxNav
595060
ChEMBL
CHEMBL1201825
Therapeutic Targets Database
DAP001260
PharmGKB
PA164746012
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ranibizumab
FDA label
Download (383 KB)
MSDS
Download (95.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingBasic ScienceNeovascular Age Related Macular Degeneration / Polypoidal Choroidal Vasculopathy (PCV)1
4Active Not RecruitingTreatmentDiabetic Macular Edema (DME)1
4Active Not RecruitingTreatmentWet Macular Degeneration1
4CompletedBasic ScienceAge Related Macular Degeneration (ARMD)1
4CompletedBasic ScienceDiabetic Macular Edema (DME)1
4CompletedBasic ScienceNeovascular Age Related Macular Degeneration1
4CompletedOtherEye Diseases / Premature Births / Retinal Diseases / Retinopathy of Prematurity Both Eyes1
4CompletedOtherNPDR - Non Proliferative Diabetic Retinopathy1
4CompletedTreatmentAge Related Macular Degeneration (ARMD)5
4CompletedTreatmentAge Related Macular Degeneration (ARMD) / Polypoidal Choroidal Vasculopathy (PCV)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Genentech Inc.
  • Novartis AG
Dosage Forms
FormRouteStrength
Injection, solutionIntravitreal
Injection, solutionIntravitreal10 mg/1mL
Injection, solutionIntravitreal10 mg/ml
Injection, solutionIntravitreal6 mg/1mL
SolutionIntravitreal10 mg / mL
Injection, solutionOphthalmic
Injection, solutionIntraocular
SolutionOphthalmic10 mg/1ml
SolutionIntraocular2.3 mg
Injection
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)Region
CA2286330No2008-06-102018-04-03Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)Not applicableFrom MSDS.
boiling point (°C)Approximately 100 degrees CFrom MSDS.
water solubilitySoluble in water.From MSDS.

Targets

Drugtargets
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Kind
Protein
Organism
Humans
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...
Gene Name
VEGFA
Uniprot ID
P15692
Uniprot Name
Vascular endothelial growth factor A
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. [Article]
  2. Michels S, Rosenfeld PJ: [Treatment of neovascular age-related macular degeneration with Ranibizumab/Lucentis]. Klin Monbl Augenheilkd. 2005 Jun;222(6):480-4. [Article]
  3. Rosenfeld PJ, Rich RM, Lalwani GA: Ranibizumab: Phase III clinical trial results. Ophthalmol Clin North Am. 2006 Sep;19(3):361-72. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Drug created on May 16, 2007 20:14 / Updated on July 29, 2021 06:27