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Ibutamoren
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Ibutamoren
Clinical data
Other namesMK-677; MK-0677; L-163,191; Oratrope
Routes of
administration		By mouth
Legal status
Legal status
Pharmacokinetic data
Elimination half-life4–6 hours (in beagles);[1] IGF-1 levels remain elevated in humans with a single oral dose for up to 24 hours[2]
Identifiers
  • 2-amino-2-methyl-N-[1-(1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxo-3-phenylmethoxypropan-2-yl]propanamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.236.734 Edit this at Wikidata
Chemical and physical data
FormulaC27H36N4O5S
Molar mass528.67 g·mol−1
3D model (JSmol)
  • O=S(C)(=O)N(C2)c1ccccc1C23CCN(CC3)C(=O)C(NC(=O)C(N)(C)C)COCc4ccccc4
  • InChI=1S/C27H36N4O5S/c1-26(2,28)25(33)29-22(18-36-17-20-9-5-4-6-10-20)24(32)30-15-13-27(14-16-30)19-31(37(3,34)35)23-12-8-7-11-21(23)27/h4-12,22H,13-19,28H2,1-3H3,(H,29,33)/t22-/m1/s1
  • Key:UMUPQWIGCOZEOY-JOCHJYFZSA-N
  (verify)

Ibutamoren (INNTooltip International Nonproprietary Name; developmental code MK-677, MK-0677, LUM-201, L-163,191; former tentative brand name Oratrope) is a potent, long-acting, orally-active, selective, and non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin.[3][4][5][6][7] It has been shown to increase the secretion of several hormones including GH and insulin-like growth factor 1 (IGF-1) and produces sustained increases in the plasma levels of these hormones while also raising cortisol levels.[8]

Effect on lean mass

[edit]

Ibutamoren has been shown to sustain activation of the GH–IGF-1 axis, increasing growth hormone secretion by up to 97%,[9] and to increase lean body mass with no change in total fat mass or visceral fat. It is under investigation as a potential treatment for reduced levels of these hormones, such as in children or elderly adults with growth hormone deficiency,[3][10][11][12] and human studies have shown it to increase both muscle mass and bone mineral density,[13][14] making it a promising potential therapy for the treatment of frailty in the elderly.[15][16] As of June 2017, ibutamoren is in the preclinical stage of development for growth hormone deficiency.[3]

Effect on sleep architecture

[edit]

In a small study of 14 subjects, ibutamoren dosed at 25 mg/day at bedtime was shown to increase rapid eye movement sleep by 20% and 50% in young and older subjects respectively.[17] Treatment with ibutamoren also resulted in an approximate 50% increase in slow-wave sleep in young subjects.[17]

Growth hormone deficiency

[edit]

In a study of children with growth hormone deficiency, ibutamoren performed better than other growth hormone secretagogues at improving growth hormone levels.[18] An ongoing study compares ibutamoren directly to injectable hGH in terms of height velocity in this population.[19] Topline data from Phase 2 OraGrowtH210 and OraGrowtH212 Trials of LUM-201 in PGHD met all primary and secondary endpoints.

Non-research use

[edit]

Since ibutamoren is still an Investigational New Drug, it has not yet been approved to be marketed for consumption by humans in the United States.[3] However, it has been used experimentally by some in the bodybuilding community. The use of ibutamoren is banned in most sports.[20]

See also

[edit]

References

[edit]
[edit]
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Ibutamoren

View on Grokipedia
from Grokipedia
Ibutamoren (also known as MK-677 or commonly MK677) is an investigational, orally active, non-peptide that acts as a selective of the receptor (GHSR). By mimicking the endogenous hormone , it stimulates pulsatile release of (GH) from the gland, leading to sustained elevations in plasma GH and (IGF-1) levels with once-daily dosing at 25 mg. This mechanism counters age-related declines in GH secretion and has been shown to improve nitrogen balance and reverse in preclinical and early human studies. Originally developed by Merck & Co. in the mid-1990s as a potential therapeutic for conditions involving GH deficiency, ibutamoren has been investigated in clinical trials for catabolic conditions. In randomized controlled trials, it has demonstrated increases in fat-free mass, GH pulsatility, and IGF-1 concentrations comparable to those in young adults, with effects persisting for up to two years of administration. More recently, under the development name LUM-201 by Lumos Pharma, it is advancing in phase 3 clinical trials as of 2025 specifically for pediatric growth hormone deficiency, aiming to provide an oral alternative to injectable GH therapies. Despite its potential benefits in enhancing and metabolic function, ibutamoren remains unapproved by the U.S. (FDA) for any indication and is classified as an unapproved drug with potential safety concerns, including elevated levels and risks of . It is prohibited by the (WADA) as a due to its ability to boost GH-related anabolic effects. Ongoing research emphasizes the need for long-term safety data, particularly regarding cardiovascular and oncogenic risks associated with prolonged GH/IGF-1 elevation.

Overview

Definition and classification

Ibutamoren is the (INN) for a synthetic compound also known by its developmental code MK-677 (commonly MK677), developed by Merck Research Laboratories as a . Its is represented by the molecular formula C27H36N4O5SC_{27}H_{36}N_{4}O_{5}S, with a molecular weight of approximately 528.67 g/mol. Ibutamoren is classified as a non-peptide, orally active that acts as a selective agonist of the receptor (GHSR). Although often misclassified or marketed as a selective androgen receptor modulator (SARM) in non-medical contexts, ibutamoren is not a SARM. This non-peptidic structure distinguishes it from earlier peptide-based secretagogues like , which have limited oral (approximately 0.3%) due to poor gastrointestinal absorption; in contrast, ibutamoren's design supports effective oral administration. Physically, ibutamoren exists as a white to off-white or beige powder, soluble in organic solvents such as (DMSO) at concentrations up to 20 mg/mL.

Development history

Ibutamoren, initially developed under the code name MK-677, originated in the 1990s at Merck & Co. as a non-peptide growth hormone secretagogue aimed at treating growth hormone (GH) deficiency and conditions involving muscle wasting, such as catabolic states. Merck's research focused on its potential as an orally active agent to stimulate GH release, building on earlier work with ghrelin mimetics. Preclinical studies in the late 1990s and early 2000s demonstrated its oral bioavailability and ability to reverse diet-induced catabolism in animal models, confirming sustained GH secretion without the need for injections. Key clinical milestones followed in the 2000s, including Phase II trials evaluating MK-677 for GH deficiency in elderly populations. A 2008 randomized trial in healthy older adults showed that 25 mg daily dosing increased GH and insulin-like growth factor-1 (IGF-1) levels, with improvements in fat-free mass over 12 months, though adverse effects like increased appetite were noted. Another Phase IIb study around 2010 assessed 25 mg/day in elderly patients, aiming to enhance recovery, but results indicated limited functional benefits. However, a Phase II trial for , completed in 2008, failed to slow cognitive decline despite elevating IGF-1 levels by up to 72.9% after 12 months, leading to discontinuation of that indication. Merck halted broader development of MK-677 in 1999 following mixed efficacy results from an early Phase III trial in pediatric GH deficiency, citing insufficient overall benefits relative to risks. Original patents filed by Merck in the mid-1990s expired in the late , opening the compound to further investigation by other entities and sparking interest in generic formulations. Following Merck's exit, companies like Ammonett Pharma briefly pursued pediatric GH deficiency applications, though a trial was terminated early due to safety concerns. As of 2025, ibutamoren remains investigational with no FDA approval for any indication; development has shifted primarily to Lumos Pharma under the name LUM-201, with ongoing Phase III trials for pediatric GH deficiency initiated in late 2025 (NCT06948214 and NCT07129759). Efforts in and frailty have seen limited progress, with prior indications discontinued due to inadequate efficacy, though exploratory studies continue in related areas like non-alcoholic .

Pharmacology

Mechanism of action

Ibutamoren, known chemically as MK-677, functions as a potent and selective non-peptide agonist of the (GHSR), also referred to as the receptor (GHSR1a), thereby mimicking the physiological effects of the endogenous peptide . This agonism occurs through high-affinity binding to GHSR, with a reported pKi value of approximately 9.3, enabling effective stimulation at low concentrations. The receptor is predominantly expressed in the and gland, where ibutamoren binding promotes the pulsatile release of (GH) from somatotroph cells in the pituitary. This GH secretion is dose-dependent; for instance, administration of 25 mg daily has been shown to increase 24-hour mean GH levels by 50-100% above baseline in clinical studies, restoring pulsatile patterns similar to those in younger individuals without inducing continuous hypersecretion due to mechanisms. Unlike some growth hormone-releasing agents, ibutamoren's action on GHSR does not significantly elevate levels, as evidenced by studies showing only minor shifts in cortisol profiles without overall increases. Downstream, the stimulated GH induces hepatic production of (IGF-1), amplifying anabolic effects, while exhibiting minimal direct influence on other pituitary hormones such as ACTH, TSH, or gonadotropins, though increases in (PRL) have been observed. Ibutamoren's prolonged duration of action stems from its high receptor affinity and slow dissociation kinetics from GHSR, which support sustained receptor activation and allow for convenient once-daily oral dosing to maintain elevated GH and IGF-1 levels over 24 hours.

Pharmacokinetics

Ibutamoren (MK-677) is administered orally and demonstrates high , estimated at more than 60% in preclinical models, enabling effective systemic exposure without parenteral administration. Absorption is rapid, with peak plasma concentrations typically achieved within 1–2 hours following ingestion, supporting its utility in once-daily regimens. The elimination of ibutamoren is approximately 4–6 hours in (with a of approximately 24 hours), though its pharmacological effects on secretion persist for up to 24 hours, facilitating sustained pulsatile release and steady-state plasma levels after 4–5 days of daily dosing. Typical research doses range from 10–25 mg per day, with 25 mg once daily being common, often administered in the evening on an empty stomach to align with natural rhythms due to its approximately 24-hour half-life. Ibutamoren undergoes primary hepatic metabolism via the enzyme , producing multiple phase I metabolites, some of which may contribute to its extended duration of action. Due to its lipophilic nature, the drug exhibits a high , allowing extensive tissue penetration, including crossing the blood-brain barrier to exert central effects on receptors. Excretion occurs predominantly via the biliary-fecal route (approximately 70% of the dose), with less than 20% renal clearance and detection of unconjugated metabolites in urine representing a smaller fraction.

Clinical effects

Effects on growth hormone and IGF-1

Ibutamoren (MK-677), an orally active receptor agonist, stimulates the to enhance endogenous (GH) secretion without significantly altering levels, distinguishing it from some other GH secretagogues. In clinical studies involving healthy adults, daily doses of 10–25 mg have increased 24-hour mean GH concentrations by 57% at 10 mg and 97% at 25 mg, reflecting a dose-dependent elevation in overall GH exposure. Peak GH pulses during these regimens have been significantly amplified, preserving and augmenting the natural pulsatile pattern of GH release, which typically diminishes with age. This effect occurs via selective activation of the (GHSR), as detailed in the section. Administration of ibutamoren consistently elevates (IGF-1) levels by 40–80%, with increases sustained over several weeks of treatment and appearing independent of age in various cohorts. For instance, a 25 mg daily dose raised serum IGF-1 by 55% after short-term use (from 141 μg/L to 219 μg/L), reaching levels comparable to those in younger adults. In elderly subjects (aged 60–81 years), short-term 25 mg/day increased IGF-1 concentrations to youthful ranges, while long-term administration (up to 2 years) sustained elevations by approximately 1.5-fold at 12 months without evidence of plateauing, indicating long-term sustainability of the hormonal response. Regarding dose-response dynamics, clinical trials demonstrate a linear relationship between ibutamoren dosage and IGF-1 elevation up to 25 mg, with simplified models from aggregated data approximating ΔIGF-1 ≈ 3 * dose (mg) in ng/mL based on observed increments (e.g., ~52% rise or 34 ng/mL at 10 mg from a ~65 ng/mL baseline). Unlike certain GH-releasing peptides, ibutamoren does not produce significant increases in ; profiles show only minor shifts in diurnal timing without overall elevation, even after repeated dosing.

Effects on body composition

Ibutamoren (MK-677) has demonstrated effects on primarily through its stimulation of the (GH)/insulin-like growth factor-1 (IGF-1) axis, leading to anabolic changes in clinical conducted in obese and elderly populations. In a phase II, randomized, double-blind, -controlled involving healthy obese males (aged 18-50 years), of 25 mg MK-677 daily for 2 months resulted in a significant increase in fat-free mass of approximately 3.0 kg compared to , as assessed by (DXA) (p < 0.01). Similar findings were observed in elderly subjects (aged 60-81 years) in a 12-month randomized, controlled , where 25 mg daily MK-677 increased fat-free mass by 1.1 kg, while the group experienced a 0.5 kg decrease (p < 0.001). These gains, typically ranging from 1-3 kg over 8-12 weeks in such cohorts, are attributed to GH/IGF-1-mediated , including enhanced nitrogen retention and protein synthesis, without direct evidence of fat-burning mechanisms. Regarding fat mass, clinical data indicate minimal or no reduction despite MK-677's appetite-stimulating effects, with outcomes varying by study population and duration. In the aforementioned 2-month trial in obese males, total body fat mass showed no significant change with MK-677 treatment, in contrast to potential gains expected from increased caloric ; this stability was linked to a concurrent 10% rise in and 24-hour energy expenditure (p < 0.05). However, in the 12-month elderly trial, fat mass increased by 1.8 kg in the MK-677 group versus 1.1 kg in (p = 0.130), representing a slight net elevation of approximately 0.7 kg relative to controls, possibly offset by metabolic improvements but not resulting in overall fat loss. Across studies, these shifts highlight MK-677's preferential impact on lean tissue over fat reduction. In diet-induced catabolic states, MK-677 preserved nitrogen balance but was associated with potential . Emerging phase 3 data in pediatric suggest sustained GH/IGF-1 increases comparable to adults, with potential benefits in growth and (as of 2025).

Effects on sleep

Ibutamoren (MK-677) enhances sleep architecture by increasing the duration of rapid eye movement (REM) sleep by 20-50% and (SWS), particularly stage IV, in both young and elderly subjects. In a clinical study of healthy young men receiving 25 mg daily for two weeks, stage IV SWS duration increased by approximately 50%, while REM sleep rose by more than 20%. In elderly participants under the same regimen, REM sleep duration increased by nearly 50%, accompanied by a significant decrease in REM latency (p < 0.02). These improvements also include enhanced sleep efficiency and fewer nocturnal awakenings, which correlate with augmented (GH) pulses during early stages, as referenced in its mechanism as a GH . Such changes contribute to overall better quality without inducing , as the compound acts through non-sedative pathways. The sleep-modulating effects stem from MK-677's activation of central receptors (GHSR) in the , which influence sleep-wake cycles independently of direct action. In the referenced studies, these benefits emerged after one week of dosing and persisted through the treatment duration without evidence of tolerance development.

Medical uses

Growth hormone deficiency

Ibutamoren (MK-677) has been investigated as an oral alternative to injectable recombinant human (rhGH) for treating (GHD) in both adult and pediatric populations, offering the advantage of stimulating endogenous GH release without the need for daily injections. In a small study of nine adults with severe GHD, oral administration of MK-677 at doses of 10 mg or 50 mg daily for four days significantly increased 24-hour mean GH concentrations by 79% and 82%, respectively, and elevated serum IGF-1 levels by 52% and 79%, respectively, restoring them toward the normal range without altering GH pulse frequency. Similarly, in children with GHD, short-term oral dosing (0.8 mg/kg/day for 7-8 days) increased peak GH, IGF-1, and IGFBP-3 levels in responders, with IGF-1 rising by up to 55% in those with moderate deficiency. Phase 2 trials of ibutamoren (as LUM-201) in pediatric GHD, such as the OraGrowtH210 trial (NCT04614337) involving children with moderate idiopathic GHD, demonstrated sustained . In OraGrowtH210, once-daily oral doses of 1.6 mg/kg led to an annualized height velocity (AHV) of 8.2 cm/year at six months, comparable to historical rhGH-treated cohorts (8.58 cm/year in year 1), with significant increases in peak stimulated GH, pulsatile GH secretion, and IGF-1 levels. A two-year extension in similar cohorts showed maintained AHV of approximately 7.0 cm/year in year 2 (reflecting a 9.9% decline from year 1), alongside improvements in scores related to physical functioning and emotional well-being, without the injection-related burden. As of November 2025, LUM-201 is advancing in an ongoing phase 3 trial (NCT06948214) for naive-to-treatment prepubertal children with moderate pediatric GHD, evaluating 12-month AHV in a multicenter, randomized, double-blind, placebo-controlled design. In healthy elderly individuals, MK-677 treatment increased IGF-1 levels 1.5-fold and enhanced pulsatile GH secretion (1.8-fold increase in 24-hour mean GH) over up to two years in exploratory studies, though development for adult GHD stalled after phase 2 due to limitations in severe cases. By mimicking the natural pulsatile pattern of GH release via ghrelin receptor agonism, ibutamoren may offer fewer side effects than continuous rhGH exposure, such as reduced risk of supraphysiological IGF-1 peaks or injection-site reactions, while improving patient adherence through oral dosing. Phase 2 data indicate comparable growth outcomes to rhGH in moderate pediatric GHD, supporting advancement to phase 3, though efficacy in severe GHD remains modest where endogenous secretion is profoundly impaired. The U.S. FDA granted orphan drug designation to ibutamoren mesylate in for GHD treatment, highlighting its potential in rare populations like elderly or hypopituitary patients.

Other potential applications

Ibutamoren has been investigated for its potential in treating and frailty among the elderly, where it may improve muscle function and reduce fall risk. In a of healthy older adults, of ibutamoren at 25 mg daily for 12 months significantly increased fat-free by approximately 1.1 kg compared to , alongside enhancements in pulsatile secretion. A phase IIb multicenter study in elderly patients recovering from hip fractures (n=123) found that 25 mg daily dosing improved functional outcomes, including stair climbing power and reduced incidence of falls, suggesting benefits for frailty-related mobility issues. In and states, ibutamoren shows promise in countering muscle loss during or chronic illness. A two-month study in healthy obese males demonstrated that 25 mg daily increased and IGF-1 levels without significant changes in body weight, indicating potential preservation of lean mass in caloric restriction. Additionally, in young men under diet-induced catabolism, ibutamoren reversed wasting, promoting anabolic effects that could extend to muscle preservation in chronic conditions. Early preclinical research has explored ibutamoren's role in Alzheimer's disease and cognitive decline, primarily through IGF-1-mediated neuroprotection. In a mouse model of Alzheimer's (5xFAD), chronic treatment with MK-0677 enhanced hippocampal neurogenesis but did not improve synaptic plasticity or cognitive performance, highlighting preliminary neuroprotective potential limited by translational challenges. For wound healing and bone health, evidence remains limited but points to accelerated post-surgical recovery. Ibutamoren treatment increased bone formation markers, such as a 23% rise in carboxy-terminal propeptide of type I procollagen and a 28% increase in procollagen III peptide, in healthy volunteers. In the aforementioned hip fracture trial, it supported faster functional recovery, though direct wound healing data is sparse. As of 2025, phase I and II trials for ibutamoren in recovery and contexts remain exploratory, with no advancement to phase III reported in recent regulatory reviews.

Non-medical use

Use in

Ibutamoren, known as MK-677, has gained popularity among bodybuilders and fitness enthusiasts as an oral (GH) booster, primarily sought for its potential to promote and enhance workout recovery. Users in these communities are motivated by its ability to stimulate GH and insulin-like growth factor 1 (IGF-1) secretion without injections, mimicking the anabolic effects associated with elevated GH levels. Typical dosing in non-medical contexts ranges from 10 to 25 mg per day, often administered in cycles lasting 8 to 12 weeks to support bulking phases or recovery periods. In circles, ibutamoren is frequently marketed online as a or , despite lacking FDA approval for human use, and is commonly stacked with selective modulators (SARMs) like LGD-4033, although ibutamoren itself is not a SARM and does not typically suppress bioavailable testosterone levels unlike many SARMs, to amplify muscle-building outcomes. Anecdotal user reports highlight enhanced muscle gains during bulking cycles and faster recovery from intense sessions, attributing these benefits to sustained GH elevation. Its prevalence in forums and online communities has grown since the , driven by the rise of performance-enhancing supplements, with sourcing typically from gray market vendors. This popularity has further extended to social media platforms like TikTok, where it is frequently promoted by influencers for bodybuilding and fitness benefits, often without adequate emphasis on the associated health risks. By 2025, ibutamoren's availability has expanded through nootropics-focused websites, where it is promoted for cognitive and performance benefits alongside fitness applications, reflecting ongoing interest despite regulatory scrutiny. These patterns underscore its appeal in unregulated fitness contexts, where users leverage its reported lean mass improvements observed in clinical settings.

Associated risks in recreational contexts

In recreational contexts, high-dose cycling of ibutamoren, often exceeding 25 mg daily for extended periods, may contribute to sustained elevation of (GH) and (IGF-1) levels, potentially increasing risks associated with chronic GH excess, such as those observed in , though no confirmed cases of symptoms like coarsening facial features, enlarged hands and feet, or joint issues have been reported with ibutamoren use. This risk arises because ibutamoren acts as a GH secretagogue, amplifying pulsatile GH release over time without the regulatory feedback present in therapeutic settings. Anecdotal reports and user reviews indicate that doses at or near 30 mg daily for approximately 8 weeks are considered high, with commonly described effects including increased lethargy, sluggishness, and more pronounced water retention compared to lower doses (e.g., 10-20 mg). These reports also frequently mention increased appetite leading to weight gain of 10-15 lbs, often involving water retention, alongside other effects such as enhanced recovery and strength gains. Such outcomes are dose-dependent, vary individually, and are not derived from controlled clinical studies. Black-market ibutamoren products, commonly sourced from unregulated vendors and marketed as dietary supplements, frequently contain contaminants or adulterants, including undeclared anabolic agents or inconsistent dosing that heightens risks. Studies on performance-enhancing supplements reveal adulteration rates of approximately 28%, where products fail to match label claims or include prohibited substances, exacerbating hazards in use. When stacked with other performance-enhancing drugs (PEDs) like anabolic steroids or selective androgen receptor modulators (SARMs), ibutamoren amplifies , as evidenced by co-administration with LGD-4033 leading to disrupted lipid profiles, worsened hepatic enzyme levels, and significant reductions in both free and total testosterone levels. This synergistic effect on can increase risk, particularly in individuals predisposed to metabolic disorders. Additionally, ibutamoren can cause a mild increase in serum prolactin levels, with studies showing a mean increase of approximately 27% from baseline after several weeks of administration, though post-treatment values remain within normal physiological ranges. Clinical trials have not reported cases of gynecomastia or breast tenderness with ibutamoren monotherapy. However, when stacked with SARMs—which can suppress endogenous testosterone production and potentially lead to relative estrogen elevation—there may be an increased risk of gynecomastia due to hormonal imbalance. Evidence for this specific risk is limited; one case report described reversible bilateral gynecomastia in a 40-year-old male using supplements containing MK-677, the SARM RAD-140, cardarine, and undisclosed hormones including testosterone, estradiol, and growth hormone, with documented normal prolactin levels, indicating that other factors (such as testosterone suppression or exogenous hormones) were likely the primary causes. The absence of medical oversight in recreational use elevates overdose risks, with doses surpassing 50 mg/day reported in user communities, far beyond studied therapeutic ranges of 10-25 mg, potentially causing severe insulin desensitization and unknown toxicities due to limited safety data. Without monitoring, acute effects like pronounced appetite stimulation—already a noted —can contribute to uncontrolled and nutritional imbalances. As of September 2025, the U.S. (FDA) issued warnings about dietary supplements containing undeclared ibutamoren, and a July 2025 documented potential associated with its use. Effects on GH and IGF-1 levels after discontinuation are generally reversible, with no evidence of dependency or rebound suppression of natural GH production.

Dosage and administration in non-medical use

Ibutamoren (also known as MK-677) is a research chemical not approved for human use by regulatory authorities. In research settings and non-medical contexts, typical dosages range from 10-25 mg per day taken orally, with 25 mg once daily being common (often at night on an empty stomach due to its approximately 24-hour effective half-life). Anecdotal user reports on online forums (primarily Reddit) indicate that some individuals administer 30 mg daily, which is considered a high dose compared to the typical range; these reports often describe more pronounced side effects at this level, such as lethargy, sluggishness, and increased water retention. Clinical studies have used daily oral doses of 5-25 mg. When supplied as powder in vials (e.g., 30 mg), accurate dosing requires weighing portions with a milligram scale or reconstituting into a solution for measured oral intake, though no standardized reconstitution protocol exists (vendors may provide guidance; common solvents include PEG-400 or ethanol). Use is for laboratory/research purposes only.

User-reported onset of effects

Anecdotal reports from users on online forums such as Reddit indicate that the onset of effects from ibutamoren (MK-677) varies considerably among individuals. Increased appetite and improved sleep quality often begin immediately or within 1–2 days to 2 weeks. Healing and recovery effects may emerge around one week. Noticeable positive effects, such as muscle growth and strength gains, typically require 1 month or longer, with some users reporting significant changes only after up to 6 months. Reports of approximately 8-week cycles (or about 2 months) at doses at or near 30 mg daily commonly describe improved sleep quality, better skin appearance, increased appetite leading to weight gain often of 10-15 pounds (including water retention), enhanced recovery, and strength gains. However, 30 mg is frequently regarded as a high dose, with some users experiencing lethargy, sluggishness, and more pronounced water retention compared to lower doses (such as 10-20 mg). Individual responses differ significantly; these are anecdotal forum reports (primarily from Reddit) and not findings from clinical studies.

Availability and sources

Ibutamoren (MK-677) is sold online as a research chemical intended for laboratory use only and is not approved by the FDA for human consumption. There are no official "best" sources due to the unregulated nature of the market, but reliable vendors typically offer third-party lab-tested products with high purity (>99%) and certificates of analysis (COAs). Popular vendors in 2026 with positive community mentions for quality and testing include Chemyo (third-party tested, >99% purity, liquid form), PureRawz (99% pure, third-party tested, various forms), and Behemoth Labz (third-party tested). Users should always verify current COAs, comply with local laws, and be aware of the risks associated with unregulated products, such as potential contamination or inconsistent quality.

Side effects and safety

Common adverse effects

Ibutamoren (MK-677) is associated with several common short-term adverse effects, primarily observed in clinical trials involving healthy older adults and individuals with . The most frequently reported effect is an increase in , occurring in 67% of participants receiving 25 mg daily compared to 36% in the group, often leading to transient of approximately 2-5 kg, largely attributable to water retention rather than fat mass. Edema, particularly mild and transient lower-extremity swelling due to fluid retention, and muscle pain are also common, affecting a notable portion of users in doses ranging from 10-25 mg daily; these effects typically resolve within weeks or upon discontinuation. Mild is another frequent occurrence, resulting in slight elevations in fasting blood glucose levels (e.g., from 5.4 to 6.8 mmol/L after 4 weeks at 25 mg) and increased insulin concentrations, though these changes are generally reversible and do not progress to clinical in short-term use. Regarding androgenic effects, unlike selective androgen receptor modulators (SARMs), ibutamoren does not typically suppress testosterone production or the hypothalamic-pituitary-gonadal axis. Available studies show possible reductions in total testosterone levels but no significant changes in free or bioavailable testosterone, with no alterations in follicle-stimulating hormone (FSH) or luteinizing hormone (LH) levels. Ibutamoren causes a mild increase in prolactin levels (typically 23-27% from baseline in short-term studies, remaining within normal physiological ranges). Clinical trials report no cases of gynecomastia or breast tenderness. The gynecomastia risk from MK-677 alone is low, as the prolactin elevation is modest and not clinically significant for most users. Additional reported effects include or , numbness or tingling in the extremities (often linked to retention), and . Transient elevations in levels have also been observed. Overall, 30-50% of trial participants experience mild adverse effects, which are dose-dependent and predominantly resolve after stopping treatment.

Long-term concerns

Prolonged use of ibutamoren (MK-677) has raised concerns regarding cardiovascular health, primarily due to its association with fluid retention and potential . Clinical trials have observed lower extremity as a common effect, which may contribute to elevated blood pressure over time, though direct causation remains under investigation. In a involving elderly hip fracture patients, ibutamoren treatment was linked to a higher incidence of congestive (4 cases in the treatment group versus 1 in ), prompting safety reevaluations in vulnerable populations. Animal models further suggest that sustained elevation of (IGF-1) from ibutamoren could promote cardiac , although human data on this mechanism is limited. The oncogenic potential of ibutamoren stems from its stimulation of the GH/IGF-1 axis, where elevated IGF-1 levels are a known for tumor promotion and progression. Epidemiological studies confirm that higher circulating IGF-1 correlates with increased incidence of several cancers, including colorectal and types, raising theoretical concerns for long-term ibutamoren users. In one two-year trial, a participant developed colon cancer following 12 months of ibutamoren exposure, though causality was not established. Due to these risks, ibutamoren is contraindicated in individuals with a history of , as the GH/IGF-1 stimulatory effects may exacerbate tumor growth. Regarding endocrine disruption, extended ibutamoren administration sustains pulsatile GH secretion without apparent desensitization of the (GHSR), as evidenced by maintained IGF-1 elevations over two years in clinical settings. However, chronic activation of the GH axis could potentially alter endogenous regulation, leading to dependency or suppression of natural GH release upon discontinuation, though in humans is sparse. This sustained perturbation may also contribute to , a concern noted in metabolic profiles during prolonged use. Sustained insulin resistance from long-term ibutamoren use may increase the risk of developing type 2 diabetes, although comprehensive long-term human studies confirming this risk and overall safety are lacking. For bone and joint health, ibutamoren initially boosts markers of bone formation, such as carboxy-terminal propeptide of type I procollagen (by 23%) and procollagen III peptide (by 28%), suggesting potential gains in the short term. Over longer durations, however, a 12-month trial reported a decline in femoral neck , indicative of heightened remodeling without net . Prolonged GH/IGF-1 elevation carries a risk of skeletal overgrowth, potentially leading to akin to acromegalic changes, though no confirmatory long-term human studies exist. Recent data from two-year clinical trials indicate no major adverse cardiovascular or oncogenic events attributable to ibutamoren, with overall tolerability favorable in healthy older adults. Nonetheless, these studies involve limited cohorts (e.g., n=65 in one crossover design), underscoring the scarcity of comprehensive long-term human evidence beyond 24 months as of late 2025.

Regulatory approval

Ibutamoren (MK-677) has not received approval from the U.S. Food and Drug Administration (FDA) for any medical use and remains classified as an unapproved substance, with ongoing investigational new drug (IND) status limiting its application to clinical research under strict protocols. As of January 2026, it remains unapproved by the FDA for any human use outside of research and is classified solely as a research chemical. As of November 2025, it is advancing in Phase 3 clinical trials under the name LUM-201 by Lumos Pharma for pediatric growth hormone deficiency. The FDA has identified significant safety risks associated with ibutamoren, including potential for congestive heart failure, and routinely issues warnings against its inclusion in unapproved products, such as dietary supplements where it appears as a hidden ingredient. In the , the (EMA) granted ibutamoren mesilate orphan drug designation in 2017 for the treatment of , and the FDA granted a similar designation in the same year, but it has not been authorized for marketing or human consumption and is restricted to investigational purposes. Similar restrictions apply in other jurisdictions, where ibutamoren is not scheduled as a controlled substance but is confined to research use due to lack of regulatory approval for therapeutic applications. Despite its unapproved status, ibutamoren is often marketed and sold online as a "" or , prompting FDA advisories since at least 2018 against human consumption due to unestablished safety and efficacy. The original patents on ibutamoren expired post-2018, eliminating exclusivity protections, yet no approvals for generic versions have been granted owing to the absence of full regulatory clearance. Globally, ibutamoren faces stringent controls; in , it is classified as a Schedule 4 prescription-only medicine but banned for sale without authorization, deemed a poison unsuitable for use outside . In , it is not authorized for any purpose, with health authorities issuing recalls and alerts for unauthorized products containing the substance due to serious health risks.

Prohibited substances in sports

Ibutamoren (MK-677) is classified as a prohibited substance by the (WADA) under section S2, Peptide Hormones, Growth Factors, Related Substances and Mimetics, specifically within the growth hormone secretagogues subcategory (S2.2.4). This prohibition has been in place since the 2008 WADA Prohibited List, which explicitly banned releasing factors for , encompassing secretagogues like ibutamoren that stimulate endogenous GH production. As a non-specified substance, it is banned at all times, both in- and out-of-competition, with no threshold for allowable use. The (USADA) and (IOC), in alignment with WADA, maintain a zero-tolerance policy toward ibutamoren. Detection occurs primarily through direct assays in urine, which identify ibutamoren and its metabolites, or indirectly via elevated (IGF-1) levels in blood serum, a downstream marker of its GH effects. Hair analysis is not a standard or routinely used method for detecting ibutamoren in anti-doping controls, which primarily rely on urine and blood samples. There is limited publicly available information from authoritative sources on the specific detection time of ibutamoren in hair for doping tests. No validated detection window in hair is widely documented in primary scientific literature or WADA resources, and no specific studies confirming long-term detection in hair for ibutamoren were identified in accessible sources. Positive findings typically result in sanctions of up to four years' ineligibility for a first violation under the World Anti-Doping Code, depending on intent and circumstances. Enforcement actions demonstrate rigorous application of these rules, with documented positive tests in competitions and (MMA). For instance, in MMA, UFC athlete received a six-month suspension in 2016 after testing positive for ibutamoren via an out-of-competition urine sample. Similar violations have occurred in events under organizations like the International Federation of Bodybuilding and Fitness (IFBB), where ibutamoren's use for has led to disqualifications and bans. As of 2025, cases continue to emerge among amateur athletes across various disciplines, underscoring enhanced testing protocols. The rationale for ibutamoren's prohibition stems from its ability to mimic effects, promoting increased , fat loss, and recovery—providing a significant unfair performance advantage without medical necessity in sports. Unlike some substances with detection thresholds, no exemption applies, reflecting concerns over its potential for abuse in high-stakes competition. In the military context, the U.S. Department of Defense (DoD) prohibits ibutamoren on its Prohibited Dietary Supplement Ingredients List as a performance-enhancing agent, barring service members from its use to maintain operational integrity and health standards.

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