AffiliationDepartment of Endocrinology, Christie Hosptial, Wilmslow Road, Manchester M20 4BX, UK.
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AbstractEpidemiological studies have highlighted the need for tight control of growth hormone (GH) and insulin-like growth factor I (IGF-I) in patients with acromegaly. Studies highlighting the events involved in GH receptor signaling have allowed the development of a pegylated GH receptor antagonist (pegvisomant) for use in humans, which has been designed to outcompete GH for the GH receptor, but which contains a position 120 amino acid substitution that prevents recruitment of a second GH receptor. This process of receptor dimerisation is crucial for signal transduction and IGF-I generation. Clinical trials of pegvisomant suggest it is the most effective treatment for acromegaly to date, as this therapy is capable of normalising serum IGF-I in up to 97% of patients when doses of 40 mg per day are used. This paper reviews the development of pegvisomant and the clinical experience in patients with acromegaly to date.
CitationPegvisomant in the treatment of acromegaly. 2003, 55 (10):1303-14 Adv. Drug Deliv. Rev.
JournalAdvanced Drug Delivery Reviews
- The place of pegvisomant in the management of acromegaly.
- Authors: Parkinson C, Trainer PJ
- Issue date: 2001 Sep
- Pegvisomant: a novel pharmacotherapy for the treatment of acromegaly.
- Authors: Paisley AN, Trainer P, Drake W
- Issue date: 2004 Mar
- Additional metabolic effects of adding GH receptor antagonist to long-acting somatostatin analog in patients with active acromegaly.
- Authors: Jawiarczyk A, Kałuzny M, Bolanowski M, Bednarek-Tupikowska G
- Issue date: 2008 Aug
- [Pegvisomant--growth hormone receptor antagonist in the treatment of acromegaly].
- Authors: Zgliczyński W, Zdunowski P
- Issue date: 2007 Sep-Oct
- Growth hormone receptor antagonists: discovery, development, and use in patients with acromegaly.
- Authors: Kopchick JJ, Parkinson C, Stevens EC, Trainer PJ
- Issue date: 2002 Oct