Description

Simple

A medication used to reduce swelling of the eye caused by various conditions, such as vessel blockage or diabetes.

Clinical

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.

Overview

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.

Pharmacology

Indication

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

Pharmacodynamic

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 s... Read more

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... Read more

Absorption

After monthly intravitreal injections, maximum serum concentrations are minimal around 0.3 ng/mL to 2.36 ng/mL.

Protein binding

Plasma protein binding is insignificant.

Volume of distribution

Volume of distribution is insignificant.

Clearance

Clearance was not quantified.

Half life

Approximately 9 days.

Route of elimination

Information currently not available.

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.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Take with or without food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abciximab
The risk or severity of adverse effects can be increased when Abciximab is combined with Ranibizumab.
Abituzumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Abituzumab.
Abrilumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Abrilumab.
Adalimumab
The risk or severity of adverse effects can be increased when Adalimumab is combined with Ranibizumab.
Adecatumumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Adecatumumab.
Aducanumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Aducanumab.
Afelimomab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Afelimomab.
Alemtuzumab
The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Ranibizumab.
Alendronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Ranibizumab is combined with Alendronic acid.
Alirocumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Alirocumab.
Amatuximab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Amatuximab.
AMG 108
The risk or severity of adverse effects can be increased when Ranibizumab is combined with AMG 108.
Anetumab ravtansine
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Anetumab ravtansine.
Anifrolumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Anifrolumab.
Anthrax immune globulin human
The 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).
Antithymocyte immunoglobulin (rabbit)
The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Ranibizumab.
Apolizumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Apolizumab.
Apomab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Apomab.
Ascrinvacumab
The risk or severity of adverse effects can be increased when Ranibizumab is combined with Ascrinvacumab.
4 References
  1. 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. 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. 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. 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