Macugen
Macugen Uses, Dosage, Side Effects, Food Interaction and all others data.
Macugen is a polynucleotide aptamer. Pegatinib aids neovascular age-related macular degeneration by binding to VEGF which in order reduces angiogenesis and vessel permeability.
Macugen was granted FDA approval on 17 September 2004.
Macugen is a selective vascular endothelial growth factor (VEGF) antagonist. VEGF is a secreted protein that selectively binds and activates its receptors located primarily on the surface of vascular endothelial cells. VEGF induces angiogenesis, and increases vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD), a leading cause of blindness. VEGF has been implicated in blood retinal barrier breakdown and pathological ocular neovascularization.
| Trade Name | Macugen |
| Generic | Pegaptanib |
| Pegaptanib Other Names | Pegaptanib Octasodium, Pegaptanib sodium |
| Weight | 0.3mg, |
| Type | Injection, Intravitreal Solution |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Pfizer Ltd |
| Available Country | Canada, India, United States, France, Netherlands, Portugal, Spain |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Macugen is a selective vascular endothelial growth factor (VEGF) antagonist used for the treatment of neovascular (wet) age-related macular degeneration.
For the treatment of neovascular (wet) age-related macular degeneration.
Macugen is also used to associated treatment for these conditions: Neovascular Age-Related Macular Degeneration
How Macugen works
VEGF-A promotes angiogenesis. Patients with certain ocular conditions, such as the wet form of age related macular degeneration (AMD), have increased levels of VEGF-A. VEGF-A, in patients with wet AMD, also increases vascular permeability and inflammation in the eye, leading to progression of the condition. Macugen is a pegylated oligonucleotide that selectively binds VEGF165, the isoform most responsible for VEGF-A's pathological action in wet AMD. This binding prevents VEGF165 from binding to its receptors, slowing or preventing further progression of wet AMD. Macugen does not inhibit VEGF121, the physiological isoform.
Toxicity
It is not known if pegaptanib is safe in pregnant women or if it is excreted in breast milk. Likewise, no studies have been done in the pediatric population. Most adverse events elated to the drug are ocular however non-ocular adverse events related to the drug or the injection procedure also occurred, among which headaches and rhinorrhoea appeared in more than 1% of patients. Macugen is contraindicated when the patient has an ocular or periocular infection.
Food Interaction
No interactions found.Volume of Distribution
It is distributed into vitreous fluid, retina, aqueous fluid, and kidneys. As well, it has been shown to cross the placenta in mice but whether or not it crosses the placenta in humans is unknown.
Elimination Route
In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration.
Half Life
In humans, after a 3 mg monocular dose (10 times the recommended dose), the average (± standard deviation) apparent plasma half-life of pegaptanib is 10 (± 4) days.
Elimination Route
It is excreted primarily in urine as unchanged drug and also as metabolites. There is no dosage adjustment required for patients with renal impairment although it must be noted that not many studies have looked at patients with a creatinine clearance of 30mL/min.
Innovators Monograph
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