Growth hormone receptor (GHR) dimerization is a prerequisite to the generat
ion 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 ant
agonist 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. (C) 20
00 Harcourt Publishers Ltd.