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Specimen Atlas of Research Peptides82 plates · MIT
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48Plate 48Reviewed 2026-07-05

MK-677

Ghrelin Receptor Agonist (oral)

also known as Ibutamoren, MK-0677, Ibutamoren Mesylate, L-163191

Orally active, non-peptide ghrelin-receptor (GHSR-1a) agonist that stimulates pulsatile growth-hormone secretion and raises IGF-1, developed by Merck as MK-0677. Unlike injectable GH secretagogues it is taken by mouth once daily. A one-year randomized trial in healthy older adults (Nass 2008) restored IGF-1 to young-adult levels and increased fat-free mass; it never reached a marketed indication despite a large clinical program. Not a peptide — a small molecule.

§ I

At a glance

Daily oral dose
25 mg
Max human evidence
Phase 2
Half-life (est)
~4–6 h
Route

Oral · Once daily

§ II

Mechanism

Edit ↗

Primary target — Ghrelin receptor (GHSR-1a) [liu-2021-ghsr].

Pathway — Ghrelin-mimetic agonism of GHSR-1a on pituitary somatotrophs → pulsatile GH release → hepatic IGF-1 production [liu-2021-ghsr][svensson-2003-mk677].

Downstream effect — Sustained IGF-1 elevation, increased fat-free mass, increased appetite; GH secretory pattern stays pulsatile [nass-2008-mk677][murphy-1998-mk677].

Origin — Small-molecule ghrelin-receptor agonist developed by Merck (MK-0677); orally bioavailable, non-peptide [philip-2022-ibutamoren].

Feedback intact — GH-axis feedback preserved — secretion remains pulsatile and subject to somatostatin, unlike exogenous GH [svensson-2003-mk677].

§ III

Dosage

Protocols described in the cited literature; not medical advice.

Edit ↗
ParameterValue
Standard dose25 mg / day oral [nass-2008-mk677]Dose used in the 1-year older-adult RCT.
FrequencyOnce daily
TimingOften taken before sleep (GH pulse + appetite) — timing is preference, not efficacy-critical
Lower / starter dose10–12.5 mg / day
Evidence basisHuman RCTs through phase IIb (e.g. hip-fracture recovery) [adunsky-2011-mk677]
DurationStudied continuously up to 12 months (Nass 2008)
FormOral capsule / solution
Half-life~4–6 h (single daily dose sustains 24-h IGF-1 elevation)
§ III · b

Reconstitution

A pure mass-to-volume utility. Enter what you have in the vial; the atlas computes the volume per dose. No prescription information.

Inputs
mg
mL
mcg
The calculator does pure mass-to-volume math. It does not recommend a dose. Refer to MK-677's cited literature for protocol specifics.
Volumetric outputFig. C — reconstitution math
Volume per dose
0.020mL
2.0 units on a U-100 insulin syringe
Concentration
12500
mcg per mL
Doses per vial
100
at this dose
§ V

Adverse events

Severities follow the FDA / CTCAE convention.

Edit ↗
Increased appetitemild
Pronounced hunger increase (ghrelin-receptor effect) — the most consistent side effect [sigalos-2018-ghs]
Fluid retention / edemamoderate
Peripheral edema, transient joint aches (GH-axis effect) [sigalos-2018-ghs]
Insulin sensitivity / glucosemoderate
Reduced insulin sensitivity and increased fasting glucose; monitor in metabolic risk [sigalos-2018-ghs]
Cortisolmild
Modest cortisol elevation reported in the class [sigalos-2018-ghs]
Hepatotoxicitysevere
Case report of drug-induced liver injury with unregulated use [cobani-2025-mk677]
No cognitive benefitmild
Raised IGF-1 but produced no cognitive benefit in an Alzheimer's RCT — IGF-1 elevation is not universally beneficial [sevigny-2008-mk677]
Absolute contraindications
  • Active malignancy (GH / IGF-1 axis stimulation)
  • Pregnancy / breastfeeding
Relative contraindications
  • Diabetes / impaired glucose tolerance (worsens insulin sensitivity)
  • Congestive heart failure or edema-prone states (fluid retention)
  • Untreated hepatic impairment
§ VI

Administration

Edit ↗
  1. 01
    Form

    Oral — capsule or solution. No reconstitution or injection.

  2. 02
    Administration

    Swallow once daily with water; food not required.

  3. 03
    Timing

    Commonly dosed before sleep; timing is a preference, not efficacy-critical.

  4. 04
    Storage

    Room temperature ≤25 °C, dry, out of light.

  5. 05
    Monitoring

    Track fasting glucose / HbA1c and signs of fluid retention with chronic use.

Appendix

Sources

38%

of 40 rendered claims carry a resolvable citation.

  1. [adunsky-2011-mk677]
    Adunsky 2011MK-0677 (ibutamoren mesylate) for the treatment of patients recovering from hip fracture: a multicenter, randomized, placebo-controlled phase IIb study
    Arch Gerontol Geriatr, 2011
  2. [cobani-2025-mk677]
    Cobani 2025Hepatotoxicity induced by MK-677
    BMJ Case Rep, 2025
  3. [liu-2021-ghsr]
    Liu 2021Structural basis of human ghrelin receptor signaling by ghrelin and the synthetic agonist ibutamoren
    Nat Commun, 2021
  4. [murphy-1998-mk677]
    Murphy 1998MK-677, an orally active growth hormone secretagogue, reverses diet-induced catabolism
    J Clin Endocrinol Metab, 1998
  5. [nass-2008-mk677]
    Nass 2008Effects of an oral ghrelin mimetic on body composition and clinical outcomes in healthy older adults
    Ann Intern Med, 2008
  6. [philip-2022-ibutamoren]
    Philip 2022Characterization of growth hormone secretagogue small molecule ibutamoren (MK-0677) and its possible metabolites in thoroughbred horses for doping control
    Rapid Commun Mass Spectrom, 2022
  7. [sevigny-2008-mk677]
    Sevigny 2008Growth hormone secretagogue MK-677: no clinical effect on AD progression in a randomized trial
    Neurology, 2008
  8. [sigalos-2018-ghs]
    Sigalos 2018The Safety and Efficacy of Growth Hormone Secretagogues
    Sex Med Rev, 2018
  9. [svensson-2003-mk677]
    Svensson 2003The effect of treatment with the oral growth hormone (GH) secretagogue MK-677 on GH isoforms
    Growth Horm IGF Res, 2003
Plate composed 2026-07-05 · maturity auto-drafted · schema v1 · Contributors: peptidesdb-core · 25 fields uncited — open contributions