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.