MUSCLE GROWTHNON-PEPTIDEResearch OnlyGROWTH HORMONE SECRETAGOGUEGHRELIN MIMETICGHSR AGONIST

MK-677

Also known as: Ibutamoren · Ibutamoren Mesylate · L-163,191 · MK-0677 · Nutrobal

38.4k views/week 214 citations 24 edits Updated 5/24/2026

MK-677 (Ibutamoren) is a potent, orally active non-peptide growth hormone secretagogue receptor (GHSR-1a) agonist that mimics ghrelin. Unlike injectable GH peptides, it provides sustained GH and IGF-1 elevation through once-daily oral dosing. Clinical trials demonstrate 40–90% IGF-1 increases, lean mass gains, improved sleep architecture, and bone density benefits at 25 mg/day. Currently the only orally bioavailable GH secretagogue with extensive human trial data.

STRUCTURE

Molecular Composition

FORMULA
C₂₇H₃₆N₄O₅S
MOL. WEIGHT
528.66 Da
CAS NUMBER
159752-10-0
TARGET
GHSR-1a (ghrelin receptor)
HALF-LIFE
~24 hours (oral)
ROUTE
Oral (once daily)
AMINO ACID CHAIN VISUALIZATION
I
Spiroindanyl
GHSR-1a hydrophobic core binding
NH-CO
B
Benzyl
Phe mimic, aromatic receptor contact
NH-CO
S
Sulfonamide
H-bond acceptor, backbone mimic
NH-CO
N
N-methyl
metabolic stability, oral bioavail.
NH-CO
P
Piperidine
basic nitrogen, ghrelin mimic
SEQUENCEI-B-S-N-P
MECHANISMS

How It Works

GHSR-1a Agonism (Ghrelin Mimicry)
MK-677 binds GHSR-1a (the ghrelin receptor) on pituitary somatotrophs and hypothalamic neurons with Ki ~1 nM — matching or exceeding endogenous ghrelin potency. This triggers phospholipase C → IP3/DAG signalling → intracellular calcium release → GH exocytosis. As a full agonist, it robustly amplifies GH pulse amplitude.
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Nocturnal GH Pulse & Sleep Architecture
GHSR-1a stimulation during slow-wave sleep (SWS) preferentially amplifies the nocturnal GH peak — the largest natural GH pulse in humans. Bedtime MK-677 significantly increases both REM and SWS duration, explaining reported improvements in sleep quality and vivid dreaming alongside the GH/IGF-1 rise.
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IGF-1 Elevation & Lean Mass
Sustained GH elevation drives hepatic IGF-1 secretion via JAK2/STAT5b. Circulating IGF-1 activates IGF-1R on muscle and bone → PI3K/Akt/mTOR (protein synthesis) and ERK1/2 (cell growth). Clinical trials show 40–90% IGF-1 increases with 1–2 kg lean mass gains over 2-year treatment in elderly adults.
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Appetite & Metabolic Effects
GHSR-1a activation in the hypothalamus (NPY/AgRP neurons) increases appetite — the most consistently reported side effect at 25 mg. Mild insulin resistance is dose-dependent and reversible. Unlike exogenous HGH, MK-677 does not cause acromegaly, organ growth, or IGF-1 elevations beyond normal physiological ranges at standard doses.
OVERVIEW

Research Overview

MK-677 (Ibutamoren) is a non-peptide small molecule developed by Merck in the 1990s using their spiroindanyl-piperidine scaffold. It is one of the most extensively studied growth hormone secretagogues (GHS) with published Phase 2 and Phase 3 human trial data spanning healthy adults, elderly populations, GH-deficient patients, and Alzheimer's disease trials.

Unlike injectable GH peptides (sermorelin, ipamorelin, CJC-1295), MK-677 is orally bioavailable, has a plasma half-life of approximately 24 hours, and can maintain elevated GH and IGF-1 levels with once-daily dosing. It does not suppress the pituitary's own GH axis — instead, it amplifies pulsatile GH secretion by mimicking ghrelin at GHSR-1a receptors in the pituitary and hypothalamus.

Its oral route, long half-life, and established safety profile make it the most practical GH secretagogue for extended research use. Phase 2 data in healthy young men showed mean IGF-1 increases of 72% at 25 mg/day after 2 weeks. In elderly adults, 2-year treatment normalized IGF-1 levels and produced significant lean mass gains (1–2 kg) without proportional fat gain — a meaningful benefit in the context of age-related sarcopenia.

Mechanism of Action

// GHSR-1a AGONISM

MK-677 binds GHSR-1a (growth hormone secretagogue receptor 1a) on pituitary somatotroph cells and hypothalamic neurons with high affinity (Ki ~1 nM). GHSR-1a activation triggers phospholipase C → IP3/DAG → intracellular calcium release → GH exocytosis. As a full agonist, MK-677 robustly amplifies GH pulse amplitude beyond physiological ghrelin levels.

// GH PULSATILITY AND SLEEP ARCHITECTURE

GHSR-1a stimulation during slow-wave sleep (SWS) preferentially amplifies the nocturnal GH pulse — the largest natural GH peak in humans. Bedtime MK-677 dosing aligns with this circadian window, significantly increasing mean nocturnal GH amplitude. Clinical sleep EEG studies confirm increased REM and SWS duration in MK-677-treated subjects — a mechanism underlying reports of enhanced sleep quality and vivid dreaming.

// IGF-1 ELEVATION AND ANABOLIC SIGNALING

Sustained GH elevation drives hepatic IGF-1 secretion via JAK2/STAT5b signaling in hepatocytes. Circulating IGF-1 binds IGF-1R on muscle, bone, and other tissues to activate PI3K/Akt/mTOR (protein synthesis, anti-catabolism) and ERK1/2 (cell proliferation). This underpins the lean mass accretion and bone density improvements in clinical trials, and explains the increase in appetite (ghrelin-mediated, via NPY/AgRP neurons).

DOSAGE

Dosage & Administration

ORAL
DOSE
10–25 mg
FREQUENCY
Once daily, preferably at night before sleep
NOTES
Bedtime dosing aligns with the natural nocturnal GH pulse and maximises slow-wave sleep enhancement. Start at 10 mg to assess appetite increase and water retention tolerance. 25 mg is the most studied dose in Phase 2 trials. Take with or without food — bioavailability is not significantly affected by meals.

MK-677 is the only orally bioavailable GH secretagogue with extensive human trial data. Its 24-hour half-life makes once-daily dosing practical. Expect increased appetite (nearly universal), mild water retention in the first 2–4 weeks, and vivid dreams. Monitor fasting glucose periodically — mild insulin resistance is dose-dependent. Not suppressive of the pituitary GH axis.

CYCLING

Cycle Duration Guide

ON CYCLE
12–24 weeks (continuous use supported by trial data)
OFF CYCLE
4–8 weeks off after extended cycles

Unlike injectable GH peptides, MK-677 does not require pulsatile dosing or short cycle periods. 2-year continuous use was studied in elderly adults with acceptable safety. For research contexts, 12–16 week cycles are common, with a washout period before resuming. IGF-1 levels should be monitored every 8–12 weeks during use.

Not approved for human therapeutic use outside clinical trials. Monitor blood glucose — mild fasting hyperglycaemia is possible, especially in insulin-resistant individuals. Not recommended for active cancer or known insulin resistance without monitoring.

NOTES

Research Notes

Phase 2 healthy young adults (Svensson et al., J Clin Endocrinol Metab, 1998): MK-677 25 mg/day × 14 days produced 72% mean IGF-1 increase vs. 2% placebo. GH 24-hour secretion rate increased 97%. No adverse effects on fasting glucose, insulin, or cortisol at this dose and duration.

Phase 2 elderly adults (Nass et al., J Clin Endocrinol Metab, 2008): 2-year randomized trial in 65+ adults. MK-677 25 mg normalized IGF-1 to young-adult levels throughout. Lean body mass increased significantly (+1.6 kg vs. baseline). Fat mass was not significantly different. Mild increase in fasting glucose and insulin resistance observed — manageable but requiring monitoring in insulin-resistant individuals.

Phase 2 hip fracture recovery: MK-677 25 mg accelerated functional recovery and reduced hospital length of stay vs. placebo, attributed to IGF-1-mediated improvement in muscle mass and bone repair.

Adverse effects: Increased appetite (nearly universal at 25 mg), mild transient edema, fatigue, mild fasting glucose elevation. Insulin resistance is dose-dependent — particularly relevant in pre-diabetic individuals. Does not suppress endogenous GH axis or cause HGH-associated side effects (acromegaly, organ growth) at standard doses.

Quick Reference
FORMULAC₂₇H₃₆N₄O₅S
MOL. WEIGHT528.66 Da
LENGTH0 amino acids
ORIGINSynthetic non-peptide small molecule (Merck); spiroindanyl-piperidine scaffold; ghrelin receptor agonist
HALF-LIFE~24 hours (oral; enables once-daily dosing)
SOLUBILITYSoluble in ethanol and DMSO; poorly soluble in water as free base; mesylate salt is more water-soluble
CAS NO.159752-10-0
STATUSResearch Only
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TAGS
growth hormone secretagogueghrelin mimeticGHSR agonistIGF-1muscle growthoralGHSsarcopeniasleep