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| Primary information |
|---|
| ID | 10556 |
| Therapeutic ID | Th1108 |
| Protein Name | Pegaptanib |
| Sequence | NA
|
| Molecular Weight | 541.6 |
| Chemical Formula | C22H44N3O10P |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | 10 ± 4 days |
| Description | It is a polynucleotide aptamer, which specifically binds to VEGF 165, a protein that plays a critical role in angiogenesis and increased permeability of blood vessels; two of the primary pathological processes responsible for vision loss associated with neovascular AMD. [Wikipedia] |
| Indication/Disease | For the treatment of neovascular (wet) age-related macular degeneration. |
| Pharmacodynamics | 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. |
| Mechanism of Action | Pegaptanib binds to the major pathological VEGF isoform, extracellular VEGF165, thereby inhibiting VEGF165 binding to its VEGF receptors. The inhibition of VEGF164, the rodent counterpart of human VEGF165, was effective at suppressing pathological neovascularization. |
| 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. |
| Metabolism | Based on preclinical data, pegaptanib is metabolized by endo- and exonucleases. |
| Absorption | In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration. |
| 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. |
| Clearance | NA |
| Categories | Intended for the prevention of respiratory distress syndrome (RDS) in premature infants at high risk for RDS. |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Vascular endothelial growth factor A |
| Brand Name | Macugen |
| Company | Gilead Sciences |
| Brand Description | Gilead Sciences |
| Prescribed For | Macugen is indicated for the treatment of neovascular (wet) age-related macular degeneration. |
| Chemical Name | NA |
| Formulation | Macugen is supplied in a single-dose, pre-filled syringe and is formulated as a 3.47 mg/mL solution, measured as the free acid form of the oligonucleotide. The active ingredient is 0.3 mg of the free acid form of the oligonucleotide without polyethylene glycol, in a nominal volume of 90 μL. This dose is equivalent to 1.6 mg of pegaptanib sodium (pegylated oligonucleotide) or 0.32 mg when expressed as the sodium salt form of the oligonucleotide moiety. The product is a sterile, clear, preservative-free solution containing sodium chloride, monobasic sodium phosphate monohydrate, dibasic sodium phosphate heptahydrate, hydrochloric acid, and/or sodium hydroxide to adjust the pH and water for injection. |
| Physical Appearance | Sterile, aqueous solution containing pegaptanib sodium for intravitreous injection |
| Route of Administration | Intravitreal Injection ONLY |
| Recommended Dosage | Macugen 0.3 mg should be administered once every six weeks into the eye to be treated. |
| Contraindication | Ocular or Periocular Infections: Macugen is contraindicated in patients with ocular or periocular infections.Hypersensitivity to pegaptanib sodium or any other excipient in this product. |
| Side Effects | The most frequently reported adverse events in patients treated with Macugen 0.3 mg for up to two years were anterior chamber inflammation, blurred vision, cataract, conjunctival hemorrhage, corneal edema, eye discharge, eye irritation, eye pain, hypertension, increased intraocular pressure (IOP), ocular discomfort, punctate keratitis, reduced visual acuity, visual disturbance, vitreous floaters, and vitreous opacities; Ocular: blepharitis, conjunctivitis, photopsia, vitreous disorder.; Non-Ocular: bronchitis, diarrhea, dizziness, headache, nausea, urinary tract infection. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |