Ibutamoren (MK-677)
Ibutamoren (MK-677) is an orally active, non-peptide growth hormone secretagogue that mimics the action of ghrelin. Research shows it can significantly increase levels of growth hormone (GH) and insulin-like growth factor 1 (IGF-1) without affecting cortisol levels, making it a subject of interest for muscle wasting, bone density, and anti-aging.
01Dosing reference
02Mechanism of action
Ghrelin receptor agonism
Binds to and activates the ghrelin receptor (GHSR-1a) in the brain.
GH and IGF-1 secretion
Stimulates the pituitary gland and hypothalamus to release growth hormone, which in turn increases IGF-1 production in the liver.
Anabolic and metabolic effects
Elevated GH and IGF-1 promote muscle protein synthesis, bone turnover, and lipolysis, offering potential benefits for frailty and muscle wasting.
03Human evidence
Increased lean body mass and basal metabolic rate.
A 2-month study in healthy older adults showed increased GH/IGF-1 and lean mass, though with transient increases in fasting blood glucose.
Reversal of diet-induced nitrogen wasting.
A short-term study in healthy young adults demonstrated that MK-677 reversed nitrogen wasting during caloric restriction.
04Preclinical evidence
Increased bone mineral density.
Animal models showed enhanced bone formation and density, suggesting potential for osteoporosis treatment.
Neuroprotective effects.
Mouse models indicated potential benefits in neurogenesis and spatial memory, likely mediated by IGF-1.
05What is known vs. unknown
- Orally bioavailable, unlike many peptide GH secretagogues.
- Increases GH and IGF-1 levels sustainably over 24 hours with a single dose.
- Does not significantly elevate cortisol or prolactin levels.
- Can increase appetite due to its ghrelin-mimetic action.
- Long-term safety regarding insulin resistance and blood glucose elevation remains a concern.
- The impact on cancer risk due to sustained elevated IGF-1 is not fully understood.
06Safety & regulatory context
07Compared with Ipamorelin
08Glossary
09Knowledge check
10Sources
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