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 chemical formula||C2158H3282N562O681S12|
|Protein average weight||48349.611 Da|
>Ranibizumab Light Chain
>Ranibizumab Heavy Chain
QSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHLDownload FASTA Format
|External Identifiers ||Not Available|
|Approved Prescription Products|
|Name||Dosage||Strength||Route||Labeller||Marketing Start||Marketing End|
|Lucentis||injection, solution||10 mg/mL||intravitreal||Genentech, Inc.||2006-06-30||Not applicable||US|
|Lucentis||solution||10 mg||intravitreal||Novartis Pharmaceuticals Canada Inc||2014-09-18||Not applicable||Canada|
|Lucentis||solution||10 mg||intravitreal||Novartis Pharmaceuticals Canada Inc||2007-07-26||Not applicable||Canada|
|Lucentis||injection, solution||6 mg/mL||intravitreal||Genentech, Inc.||2012-08-10||Not applicable||US|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products ||Not Available|
|International Brands||Not Available|
|Brand mixtures||Not Available|
|Super Class||Organic Acids|
|Class||Carboxylic Acids and Derivatives|
|Sub Class||Amino Acids, Peptides, and Analogues|
|Alternative Parents||Not Available|
|Molecular Framework||Not Available|
|External Descriptors||Not Available|
|Indication||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.|
|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 was not quantified.
|Route of elimination||Not Available|
|Half life||Approximately 9 days.|
Clearance was not quantified.
|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.
|SNP Mediated Effects||Not Available|
|SNP Mediated Adverse Drug Reactions||Not Available|
|Injection, solution||intravitreal||10 mg/mL|
|Injection, solution||intravitreal||6 mg/mL|
|Lucentis 0.5 mg vial||2340.0USD ||vial|
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
|Patent Number||Pediatric Extension||Approved||Expires (estimated)|
|melting point||Not applicable||From MSDS.|
|boiling point||Approximately 100 degrees C||From MSDS.|
|water solubility||Soluble in water.||From MSDS.|
|Synthesis Reference||Not Available|
- 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 ]
- 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 ]
- 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 ]
- 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 ]
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Download (383 KB) |
|MSDS||Download (95.8 KB) |
|Belimumab||The risk or severity of adverse effects can be increased when Ranibizumab is combined with Belimumab.|