Mimics ghrelin to stimulate pulsatile GH release and sustained IGF-1 elevation. 24-hour oral half-life enables once-daily dosing. Does not significantly affect cortisol. Note: not a peptide in the strict biochemical sense — it is a small-molecule ghrelin mimetic.
Off-label: GH optimization, body composition, sarcopenia (elderly), anti-aging. Oral administration advantage over injectable GH secretagogues.
Diabetes/insulin resistance (raises fasting glucose). Active malignancy. Edema-sensitive conditions.
2-year RCT confirms GH/IGF-1 restoration and FFM increase. Failed in Alzheimer's trial despite IGF-1 normalization (NEGATIVE).
- 1.Nass R et al., Ann Intern Med 2008 — 2-year RCT: restored GH/IGF-1 to young-adult levels. FFM increased +1.1kg. n=65, Phase II RCT
- 2.Sevigny JJ et al., Neurology 2008 — NO clinical effect on AD progression despite raising IGF-1. NEGATIVE. n=563, Phase II RCT
Not FDA-approved despite extensive study. FFM gains may partly reflect intracellular water. Raises fasting glucose and worsens insulin sensitivity. Failed in Alzheimer's trial.
LUM-201 (oral ibutamoren formulation) in Phase II for pediatric GH deficiency. Sarcopenia and frailty applications in elderly.