|Drug class||Growth hormone receptor blocker|
|Side effects||Headache, diarrhea, joint pain|
|Chemical and physical data|
|Molar mass||22 129 g·mol−1 (unpegylated)|
Pegvisomant, sold under the brand name Somavert, is a medication used to treat acromegaly. It maybe used when the condition is not controlled by surgery, radiation therapy and somatostatins. It is given by injection under the skin.
Most side effects are mild to moderate. Common side effects include headache, diarrhea, and joint pain. Other side effects may include liver problems and low blood sugar. While there is no evidence of harm in pregnancy, such use has not been well studied. It is a growth hormone receptor blocker.
Pegvisomant was approved for medical use in Europe in 2002 and the United States in 2003. In the United Kingdom it costs the NHS about £1,500 a month at 10 mg per day as of 2021. This amount in the United States is about 7,500 USD.
Long-term treatment studies with pegvisomant as a monotherapy have shown it to be safe, and to date it is the most effective treatment of acromegaly as both a monotherapy and in combination with somatostatin analogues.
It is started at a dose of 80 mg, 10 mg per day is than given which may be increased up to 30 mg per day.
Mechanism of action
Pegvisomant blocks the action of growth hormone on the growth hormone receptor to reduce the production of IGF-1. IGF-1 is responsible for most of the symptoms of acromegaly, and the normalization of its levels can control the symptoms.
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 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.
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