Pegvisomant
| Clinical data | |
|---|---|
| Trade names | Somavert |
| AHFS/Drugs.com | Monograph |
| ATC code | H01AX01 (WHO) |
| Identifiers | |
| CAS Number |
218620-50-9 
|
| IUPHAR/BPS | 7485 |
| DrugBank |
DB00082 
|
| ChemSpider | none |
| UNII |
N824AOU5XV
|
| KEGG |
D05394
|
| ChEMBL |
CHEMBL1201515
|
| Chemical and physical data | |
| Formula | C990H1532N262O300S7 |
| Molar mass | 22129.0 g/mol (unpegylated) |
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Pegvisomant (trade name Somavert) is a growth hormone receptor antagonist used in the treatment of acromegaly. It is primarily used if the pituitary gland tumor causing the acromegaly cannot be controlled with surgery or radiation, and the use of somatostatin analogues is unsuccessful; but is also effective as a monotherapy. It is delivered as a powder that is mixed with water and injected under the skin.
Pegvisomant was discovered at Ohio University in 1987 by Distinguished Professor John Kopchick and graduate student Wen Chen at the Edison Biotechnology Institute. After completing clinical trials, it was approved for the treatment of acromegaly by the FDA in 2003 and marketed by Pfizer.
Pegvisomant is a protein containing 191 amino acid residues to which several polyethylene glycol polymers have been covalently bound in order to slow clearance from the blood. The protein is a modified version of human growth hormone designed to bind to and block the growth hormone receptor. It is manufactured using genetically modified E. coli bacteria.
Pegvisomant blocks the action of growth hormone at the growth hormone receptor to reduce the production of IGF-1. IGF-1 is responsible for most of the symptoms of acromegaly, and normalising its levels may control the symptoms.
Long-term treatment studies with pegvisomant as a monotherapy have shown it be safe, and to date is the most effective treatment of acromegaly as both a monotherapy and in combination with somatostatin analogues.
Side effects of Pegvisomant include reactions at the injection site, swelling of the limbs, chest pain, hypoglycemia, nausea and hepatitis.
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