Ranibizumab

Products

Ranibizumab is commercially available as a solution for injection (Lucentis). The drug was approved in the United States and many countries in 2006 and in the EU in 2007. The drug’s high price is controversial, especially when compared with bevacizumab (Avastin), which is structurally and pharmacologically similar. Bevacizumab is not approved for these indications but is used off-label.

Structure and Properties

Ranibizumab is a Fab antibody fragment of an IgG1κ monoclonal antibody against VEGF-A (human vascular endothelial growth factor A). The fragment has a molecular weight of approximately 48 kDa and is produced by biotechnological methods. Ranibizumab is derived from the same antibody used to make bevacizumab.

Effects

Ranibizumab (ATC S01LA04) binds to VEGF-A, inhibiting activation of the receptors VEGFR-1 and VEGFR-2. VEGF-A plays an important role in endothelial cell proliferation, fluid leakage from vessels, and new vessel formation. Its half-life in the vitreous is estimated to be approximately nine days.

Indications

For treatment:

  • Of exudative (wet) age-related macular degeneration (wet AMD).
  • Of active choroidal neovascularization (CNV) affecting visual acuity.
  • Of a loss of visual acuity due to choroidal neovascularization (CNV) resulting from pathologic myopia (PM).
  • Of a loss of visual acuity due to diabetic macular edema (DME).
  • Of a loss of visual acuity due to macular edema resulting from retinal vein occlusion (retinal branch retinal vein occlusion BRVO and retinal central retinal vein occlusion CRVO).

Dosage

According to the drug label. Ranibizumab is injected directly into the vitreous of the eye under aseptic conditions after local anesthesia. The injection is usually given once a month.

Contraindications

  • Hypersensitivity
  • Infections in or around the eye
  • Intraocular inflammation

Refer to the drug label for complete precautions.

Interactions

Drug-drug interactions are not known.

Adverse effects

The most common possible adverse effects include local reactions in the eye such as inflammation, visual disturbances, eye pain, retinal disorders, and mouches volantes. Systemic adverse effects are also possible, most commonly nasopharyngitis, headache, and joint pain. Ranibizumab increases the risk of arterial thromboembolic events.