Pegvisomant: a growth hormone receptor antagonist for the treatment of acromegaly.
Growth hormone receptor (GHR) dimerization is a prerequisite to the generation of growth hormone (GH) action. Pegvisomant is a GHR antagonist that has been designed to bind to the GHR at the cell surface and hence block this process. Initial studies suggest that pegvisomant is a highly effective antagonist of GH action in patients with acromegaly. The blockade of GH action, rather than the inhibition of pituitary GH secretion, represents a novel concept in the medical management of acromegaly. In this review, the design, efficacy, challenges and future role of pegvisomant are discussed.
Parkinson
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Department of Endocrinology, Christie Hospital, Manchester, UK.
Trainer
P J
PJ
D000172:Acromegaly / Q000188:drug therapy*; D000818:Animals; D000917:Antibody Formation; D001665:Binding Sites; D019281:Dimerization; D005260:Female; D000882:Haplorhini; D019382:Human Growth Hormone / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D008954:Models, Biological; D051381:Rats; D011986:Receptors, Somatotropin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015398:Signal Transduction
D011986:Receptors, Somatotropin; D019382:Human Growth Hormone; C406545:pegvisomant