Pegaptanib

Pegaptanib Uses, Dosage, Side Effects, Food Interaction and all others data.

Pegaptanib is a polynucleotide aptamer. Pegatinib aids neovascular age-related macular degeneration by binding to VEGF which in order reduces angiogenesis and vessel permeability.

Pegaptanib was granted FDA approval on 17 September 2004.

Pegaptanib 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 Pegaptanib
Generic Pegaptanib
Pegaptanib Other Names Pegaptanib Octasodium, Pegaptanib sodium
Weight 0.3mg
Type Intraocular, Intravitreal Solution
Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Pegaptanib
Pegaptanib

Uses

Pegaptanib 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.

Pegaptanib is also used to associated treatment for these conditions: Neovascular Age-Related Macular Degeneration

How Pegaptanib 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. Pegaptanib 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. Pegaptanib 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. Pegaptanib 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

You find simplified version here Pegaptanib

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