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Effects of oral administration of ibutamoren mesylate

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Ibutamoren mesylate (MK-0677), an orally active nonpeptide growth  hormone (GH) secretagogue, stimulates GH release through a pituitary and  hypothalamic receptor that is different from the GH-releasing hormone  receptor. We evaluated the safety and tolerability and the  GH-insulin-like growth factor (IGF) responses to two dosages of oral  ibutamoren mesylate given to children with GH deficiency for 7 to 8  days. The patients, 18 prepubertal children (15 male, 3 female) with  idiopathic GH deficiency, had a chronologic age of 10.6 +/- 0.8 years  (mean +/- SD), bone age of 7.4 +/- 0.7 years, growth velocity < 10th  percentile for age, height < 10th percentile for age, and a maximum  GH response of < or = 10 microg/L to two different GH stimulation  tests. The children were assigned as follows to one of three treatment  groups with ibutamoren mesylate: 0.2 mg/kg per day for 7 days (days 1-7  or 8-14) and matching placebo for the alternate 7 days (groups I and II,  respectively) or 0.8 mg/kg per day for 7 days (days 8-14, group III).  On day 15 all patients received an 0.8-mg/kg dose of ibutamoren  mesylate. Patients in groups I and II were studied first to assess  safety at the low dose before advancement to the high dose. Hormonal  profiles were evaluated on day -1 (baseline) and day 15, and the results  were expressed as the change from baseline within each group. After  administration of ibutamoren mesylate 0.8 mg/kg for 8 days (group III),  the median increases (on day 15) from baseline were as follows: 3.8  microg/L (range, 0 to 34.3) for serum GH peak concentration (P = .001),  4.3 microg x h/L (range, 1.3 to 35.6) for the GH area under the  concentration-time curve from time zero to 8 hours (AUC(0-8)) (P <  .001), 12 microg/L (range, -4 to 116) for serum IGF-I (P = .01), and 0.4  microg/L (range, -0.9 to 1.5) for serum IGF-binding protein 3 (IGFBP-3)  (P = .01). There was no change in serum prolactin, glucose,  triiodothyronine, thyroxine, thyrotropin, peak serum cortisol, and  insulin concentrations or 24-hour urinary free cortisol after  administration of 0.8 mg/kg per day of ibutamoren mesylate for 8 days.  We conclude that short-term administration of ibutamoren mesylate can  increase GH, IGF-I, and IGFBP-3 levels in some children with GH  deficiency. Thus this compound is applicable for testing its effect on  growth velocity. 

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