Growth hormone receptor antagonist. Genetically engineered analog of human growth hormone conjugated to polyethylene glycol (PEG), q.v., to improve bioavailability. Prepn: B. C. Cunningham et al., WO 9711178; eidem, US 5849535 (1997, 1998 both to Genentech). Receptor binding and effects of pegylation on structure and function: R. J. M. Ross et al. J. Clin. Endocrinol. Metab. 86, 1716 (2001). Clinical pharmacology: M. O. Thorner et al., ibid. 84, 2098 (1999). Clinical trial in acromegaly: P. J. Trainer et al., N. Engl. J. Med. 342, 1171 (2000); A. J. van der Lely et al., Lancet 358, 1754 (2001). Review of clinical experience: C. Parkinson, P. J. Trainer, Expert Opin. Invest. Drugs 10, 1725-1735 (2001); of structure and function: S. Pradhananga et al., J. Mol. Endocrinol. 29, 11-14 (2002); of preclinical and clinical development: V. Goffin, P. Touraine, Curr. Opin. Investig. Drugs 5, 463-468 (2003).
In treatment of acromegaly.
Growth Hormone Antagonist/Inhibitor