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Review
. 2002 Oct;23(5):623-46.
doi: 10.1210/er.2001-0022.

Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly

J J Kopchick  1 , C Parkinson, E C Stevens, P J Trainer
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Review

Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly

J J Kopchick et al. Endocr Rev. 2002 Oct.

Abstract

An understanding of the events that occur during GH receptor (GHR) signaling has facilitated the development of a GHR antagonist (pegvisomant) for use in humans. This molecule has been designed to compete with native GH for the GHR and to prevent its proper or functional dimerization-a process that is critical for GH signal transduction and IGF-I synthesis and secretion. Clinical trials in patients with acromegaly show GHR blockade to be an exciting new mode of therapy for this condition, and pegvisomant may have a therapeutic role in diseases, such as diabetes and malignancy, in which abnormalities of the GH/IGF-I axis have been observed. This review charts the discovery and development of GHR antagonists and details the experience gained in patients with acromegaly.

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