Ipamorelin
Ipamorelin is a synthetic pentapeptide ghrelin receptor (GHSR1a) agonist and selective growth hormone secretagogue originally characterized for its highly selective GH-releasing properties with minimal off-target hormonal effects [1]. Human pharmacokinetic data from a controlled study demonstrate a short terminal half-life of approximately 2 hours and dose-proportional kinetics across a range of intravenous doses [2]. Outside of a phase II randomized controlled trial in postoperative ileus [3], human efficacy data are absent, and most mechanistic evidence derives from animal and in vitro models.
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1 claim pending coverage
- FDA prescribing-label data(1 claim)
Pepteligence regenerates entries quarterly and when new high-tier evidence appears.
Quick facts
Suggested labs for this peptide class — educational reference only; not medical advice.
TL;DR
- Half-life: — — dosed —.
- Administered via multiple.
- Evidence base: randomised controlled trials.
- Primary goals: growth-hormone, gh-release.
Randomised controlled trials
How it works
Ipamorelin is a pentapeptide agonist at the ghrelin receptor subtype GHSR1a, acting as a selective growth hormone secretagogue [1]. In vitro studies using rat pituitary cells demonstrated that ipamorelin stimulates GH release with an EC50 of 1.3 ± 0.4 nmol/L and an Emax of 85 ± 5%, indicating potent and near-maximal efficacy at the receptor [1]. Unlike earlier growth hormone secretagogues, ipamorelin was characterized as the first selective GHS, showing minimal stimulation of cortisol, prolactin, or ACTH release in preclinical models [1]. Mechanistic data indicate that ipamorelin's GH-releasing effects are mediated through the GHSR1a pathway [12], and animal studies indicate that chronic ipamorelin treatment alters somatotroph cell populations and GH content in rat pituitary tissue [13]. Animal studies further indicate that ipamorelin acts as a peripherally restricted ghrelin receptor agonist capable of attenuating visceral and somatic pain in experimental models of non-inflammatory hypersensitivity and mechanical allodynia [8]. Animal studies also suggest GH-independent effects on adiposity: ipamorelin increased fat pad weights relative to body weight in both GH-deficient and GH-intact mouse models, pointing to direct adipogenic signaling independent of the GH axis [7]. In streptozotocin-diabetic mice, intravenous ipamorelin induced GH hypersecretion (GH levels 150 ± 35 µg/L versus 62 µg/L in controls) alongside reduced hepatic IGF-I mRNA expression, suggesting altered downstream signaling in a diabetic metabolic context [11]. Animal studies indicate that ipamorelin inhibited cisplatin-induced weight loss in ferrets at doses of 1–3 mg/kg administered intraperitoneally, an effect shared with the related ghrelin mimetic anamorelin, which additionally demonstrated anti-emetic properties via a central mechanism [9]. These mechanistic findings are derived entirely from in vitro and animal models; their relevance to human physiology has not been established in controlled clinical trials.
What the research says
Research summary content coming soon. Check the references section for indexed studies.
Protocol lifecycle
Before — Pre-cycle readiness
Readiness checklist
Regulatory and legal
Medical evaluation
- Obtain baseline endocrine panel including IGF-1 and fasting glucose given animal data showing GH hypersecretion and altered IGF-I mRNA in diabetic models [11].
- Discuss with a licensed clinician; no published human dosing or safety guidance exists beyond a small pharmacokinetic study (n=8 per dose level) [2].
Evidence awareness
- Acknowledge that all efficacy claims for muscle growth, fat loss, recovery, or pain management in humans lack clinical trial evidence — these are extrapolated from animal and in vitro studies only [8], [9].
- Understand that modified ipamorelin analogs exist in unregulated markets with unknown safety profiles [6].
- Confirm ipamorelin is not prohibited in your jurisdiction or sport; it is on the WADA Prohibited List [4].
- Assess baseline metabolic and endocrine status — animal data suggest potential GH-independent adipogenic effects that may be relevant in certain metabolic phenotypes [7].
- Note that no human data establish a safe starting dose outside the investigational pharmacokinetic study context [2].
During — Active protocol
- Human pharmacokinetic data confirm dose-proportional kinetics across intravenous doses from 4.21 to 140.45 nmol/kg over 15 minutes in a controlled research setting [2]; extrapolation to subcutaneous or intranasal community use is not supported by published evidence.
- The only published human efficacy trial evaluated ipamorelin for postoperative ileus in bowel resection patients; outcomes from this phase II RCT are the sole clinical human efficacy data available [3].
- Monitor for any signs consistent with GH-axis perturbation; no human safety monitoring guidance exists beyond the single pharmacokinetic study [2].
After — Post-cycle
- [insufficient evidence in research packet — no human data on cycling, washout, or post-cycle management for ipamorelin]
Stacks it appears in
Ipamorelin is typically used as a standalone compound. Stack data coming soon.
Related peptides
Other compounds indexed on Pepteligence that share research tags with Ipamorelin. Educational context only.
Safety
Common side effects
- ·[insufficient evidence in research packet — no systematic adverse event frequency data from human trials]
Rare side effects
- ·[insufficient evidence in research packet]
- Animal studies indicate GH-independent adipogenic signaling that could theoretically alter cardiometabolic risk parameters; not studied in humans [7].
- GH hypersecretion observed in a diabetic animal model suggests potential for dysregulated GH axis activity in metabolically compromised individuals [11].
Contraindications
- ·Competitive athletes subject to WADA or equivalent anti-doping authority testing — ipamorelin is prohibited in sport [4].
- ·Conditions associated with altered GH/IGF-I axis sensitivity (e.g., diabetes mellitus) based on animal model data showing GH hypersecretion and reduced hepatic IGF-I mRNA; clinical relevance in humans not established [11].
- ·Pregnancy, lactation, and pediatric populations — no safety data available in the research packet.
Community experiences
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Ipamorelin — at a glance
| Property | Ipamorelin | — |
|---|---|---|
| Half-life | — | — |
| Route | multiple | — |
| Typical dose | See research context | — |
| Mechanism | Ipamorelin is a pentapeptide agonist at the ghrelin receptor subtype GHSR1a, acting as a selective growth hormone secretagogue. In vitro studies using rat pituitary cells demonstrated that ipamorelin stimulates GH release with an EC50 of 1.3 ± 0.4 nmol/L and an Emax of 85 ± 5%, indicating potent and near-maximal efficacy at the receptor. Unlike earlier growth hormone secretagogues, ipamorelin was characterized as the first selective GHS, showing minimal stimulation of cortisol, prolactin, or ACTH release in preclinical models. Mechanistic data indicate that ipamorelin's GH-releasing effects are mediated through the GHSR1a pathway, and animal studies indicate that chronic ipamorelin treatment alters somatotroph cell populations and GH content in rat pituitary tissue. Animal studies further indicate that ipamorelin acts as a peripherally restricted ghrelin receptor agonist capable of attenuating visceral and somatic pain in experimental models of non-inflammatory hypersensitivity and mechanical allodynia. Animal studies also suggest GH-independent effects on adiposity: ipamorelin increased fat pad weights relative to body weight in both GH-deficient and GH-intact mouse models, pointing to direct adipogenic signaling independent of the GH axis. In streptozotocin-diabetic mice, intravenous ipamorelin induced GH hypersecretion (GH levels 150 ± 35 µg/L versus 62 µg/L in controls) alongside reduced hepatic IGF-I mRNA expression, suggesting altered downstream signaling in a diabetic metabolic context. Animal studies indicate that ipamorelin inhibited cisplatin-induced weight loss in ferrets at doses of 1–3 mg/kg administered intraperitoneally, an effect shared with the related ghrelin mimetic anamorelin, which additionally demonstrated anti-emetic properties via a central mechanism. These mechanistic findings are derived entirely from in vitro and animal models; their relevance to human physiology has not been established in controlled clinical trials. | — |
| Evidence strength | rct | anecdotal |
| Primary goal | growth-hormone | — |
Frequently asked questions
What is ipamorelin?
How does ipamorelin work?
What is ipamorelin used for?
Is ipamorelin FDA-approved?
What are common dosages of ipamorelin?
How is ipamorelin administered?
What are common side effects of ipamorelin?
Is ipamorelin prohibited in competitive sports?
Are there concerns about ipamorelin and diabetes or metabolic conditions?
Can ipamorelin be combined with other peptides?
Is ipamorelin legal?
How does ipamorelin differ from MK-677?
References
- [1]
Ipamorelin, the first selective growth hormone secretagogue.
Raun K, Hansen B S, Johansen N L et al.
European Journal of Endocrinology · 1998 · PMID 9849822
View on PubMed → - [2]
Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers.
Gobburu J V, Agersø H, Jusko W J et al.
Pharmaceutical Research · 1999 · PMID 10496658
View on PubMed → - [3]
Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients.
Beck David E, Sweeney W Brian, McCarter Martin D et al.
International Journal of Colorectal Disease · 2014 · PMID 25331030
View on PubMed → - [4]
A new era of doping? Use of peptide and peptide-analog drugs in recreational and professional sport and bodybuilding: a critical review.
Coutinho Luis F D, DE Oliveira Neves Lucas F, Camilo Rafael P
The Journal of Sports Medicine and Physical Fitness · 2026 · PMID 41880199
View on PubMed → - [5]
Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin.
Semenistaya Ekaterina, Zvereva Irina, Thomas Andreas et al.
Drug Testing and Analysis · 2015 · PMID 25869809
View on PubMed → - [6]
Glycine-modified growth hormone secretagogues identified in seized doping material.
Gajda Paulina Marta, Holm Niels Bjerre, Hoej Lars Jakobsen et al.
Drug Testing and Analysis · 2019 · PMID 30136411
View on PubMed → - [7]
Growth hormone (GH)-independent stimulation of adiposity by GH secretagogues.
Lall S, Tung L Y, Ohlsson C et al.
Biochemical and Biophysical Research Communications · 2001 · PMID 11162489
View on PubMed → - [8]
Attenuation of Visceral and Somatic Nociception by Ghrelin Mimetics.
N Mohammadi Ehsan, Louwies Tijs, Pietra Claudio et al.
Journal of Experimental Pharmacology · 2020 · PMID 32801950
View on PubMed → - [9]
The growth hormone secretagogue receptor 1a agonists, anamorelin and ipamorelin, inhibit cisplatin-induced weight loss in ferrets: Anamorelin also exhibits anti-emetic effects via a central mechanism.
Lu Zengbing, Ngan Man P, Liu Julia Y H et al.
Physiology & Behavior · 2024 · PMID 39043357
View on PubMed → - [10]
Analysis of new growth promoting black market products.
Krug Oliver, Thomas Andreas, Malerød-Fjeld Helle et al.
Growth Hormone & IGF Research · 2018 · PMID 29864719
View on PubMed → - [11]
Growth hormone (GH) hypersecretion and GH receptor resistance in streptozotocin diabetic mice in response to a GH secretagogue.
Johansen Peter B, Segev Yael, Landau Daniel et al.
Experimental Diabesity Research · 2003 · PMID 14630569
View on PubMed → - [12]
Pharmacological characterisation of a new oral GH secretagogue, NN703.
Hansen B S, Raun K, Nielsen K K et al.
European Journal of Endocrinology · 1999 · PMID 10427162
View on PubMed → - [13]
Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro.
Jiménez-Reina L, Cañete R, de la Torre M J et al.
Histology and Histopathology · 2002 · PMID 12168778
View on PubMed → - [?]
The influence of ghrelin agonist ipamorelin acetate on the hypothalamic-pituitary-testicular axis in a cichlid fish, Oreochromis mossambicus.
Gouda Mallikarjun, Ganesh C B
Animal Reproduction Science · 2024 · PMID 38996787
View on PubMed →