218620-50-9

Basic information

• Product Name: Pegvisomant
• Synonyms: Pegvisomant
• CAS NO: 218620-50-9
• Molecular Formula: C257H383N65O77S6
• Molecular Weight: 5807.57022
• Mol File: 218620-50-9.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Pegvisomant(CAS DataBase Reference)
• NIST Chemistry Reference: Pegvisomant(218620-50-9)
• EPA Substance Registry System: Pegvisomant(218620-50-9)

Safety Data

• Hazardous Substances Data: 218620-50-9(Hazardous Substances Data)

Usage

Description

Pegvisomant, also known as Somavert, is a PEGylated form of a recombinant human growth hormone (GH) antagonist (B2036). It is a modified form of human GH that acts as a highly selective GH receptor antagonist, specifically designed for the treatment of acromegaly.

Uses

Used in Pharmaceutical Industry:
Pegvisomant is used as a therapeutic agent for the treatment of acromegaly. It functions through competitive inhibition of peripheral growth hormone receptors to block insulin-like growth factor I (IGF-I) production. This treatment is particularly beneficial for patients with acromegaly, a rare debilitating endocrine disease caused by excessive secretion of growth hormone and increased production of IGF-I.
The clinical manifestations of uncontrolled acromegaly include soft-tissue swelling, joint pain, nerve entrapment, glucose intolerance, hypertension, and cardiac disease. Pegvisomant selectively binds to GH receptors on cell surfaces, blocking the binding of endogenous GH and interfering with GH signal transduction, which leads to a decrease in serum concentrations of IGF-I.
Clinical studies have shown that daily treatment with pegvisomant can normalize IGF-I concentrations in a significant percentage of patients, with a recommended dosage regimen of a 40 mg loading dose, followed by a 10 mg daily dose administered subcutaneously. Pegvisomant is generally well tolerated, with common side effects including injection-site reactions, diarrhea, nausea, chest pain, and flu-like symptoms.
Pegvisomant has been designated as an Orphan Drug by the FDA for the treatment of acromegaly, highlighting its importance in addressing a rare and debilitating condition with limited treatment options.

Originator

Sensus (Pfizer) (US)

Biological Functions

This product contains 191 amino acid residues (of recombinant origin), the same number as in GH, but there are substitutions at residues 18, 21, 120, 167, 168, 171, 172, 174, and 179. This product is then covalently linked to several polyethylene glycol molecules, and this pegylated protein is a GH-receptor antagonist. Thus, pegvisomant binds to the GH receptor and blocks endogenous GH from binding. The result is a blocking of the GH-stimulated overproduction of IGF-I that contributes to the disabling symptoms and long-term health problems associated with acromegaly.