Ipamorelin Research

Research

Ipamorelin research studies database

Every indexed ipamorelin record with model, route, what was measured, limitations and evidence grade. Search and filter by model, domain or year.

By the Ipamorelin Research editorial team · Last reviewed · Scientific review: pending

Short answer

This database holds every one of the 55 records returned by a PubMed search for ipamorelin and NNC 26-0161, each classified by research model, the substance actually tested, what was measured and its limitations. 42 are primary studies and 13 are reviews or commentary. Reviews are never counted as evidence.

What is in the database

By evidence grade

A: randomised controlled human trial
1
B: other human study (no control group, or not randomised)
2
C: animal study (in vivo)
21
D: cell, tissue, receptor or analytical study
18
R: review or commentary (context, not evidence)
13

By research model

Human study
3
Animal study (in vivo)
21
Ex vivo (excised tissue; no animal received the substance)
1
In vitro (cells or receptor preparations)
6
Analytical chemistry
11
Review or commentary
13

Of the 42 primary records, 12 have ipamorelin itself as their subject. The rest test an analogue built from the ipamorelin scaffold, include ipamorelin among several compounds compared, or analyse market product. That distinction is a filter in the explorer, because a finding for NN703 or Gly-ipamorelin is not a finding for ipamorelin. The search that produced the corpus returned 55 records, all of which are indexed [PubMed search], spanning 1998 to 2026.

Search and filter

Filters are reflected in the address bar, so any filtered view can be copied and shared. Selecting records and choosing “compare” opens them side by side in the study comparison tool. Citations can be exported as RIS, BibTeX or plain text.

Model
Evidence grade
What was studied
Substance tested

55 of 55 records

  • 2026 · Am J Sports Med · Review or commentary · Grade R

    Injectable Peptide Therapy: A Primer for Orthopaedic and Sports Medicine Physicians

    Mayfield CK, Bolia IK, Feingold CL et al.

    Model and system
    Narrative review · No organism dosed
    Design
    Narrative review for orthopaedic and sports medicine physicians
    What was measured
    The 2026 review evaluated current evidence and applications of injectable peptide therapy in regenerative medicine and sports performance.
    Reported findings
    Reported as a primer on the current evidence base.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · J Am Acad Orthop Surg Glob Res Rev · Review or commentary · Grade R

    Therapeutic Peptides in Orthopaedics: Applications, Challenges, and Future Directions

    Rahman OF, Lee SJ, Seeds WA

    Model and system
    Narrative review · No organism dosed
    Design
    Narrative review of therapeutic peptides in orthopaedics
    What was measured
    The 2026 review described signalling pathways attributed to therapeutic peptides and grouped ipamorelin with other secretagogues said to activate IGF-1 signalling and satellite cell repair.
    Reported findings
    Reported as a mechanistic overview rather than an outcome synthesis.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review. The mechanistic statements are broad and are not traceable to ipamorelin-specific primary studies within the review itself.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · J Sports Med Phys Fitness · Review or commentary · Grade R

    A new era of doping? Use of peptide and peptide-analog drugs in recreational and professional sport and bodybuilding: a critical review

    Coutinho LFD, DE Oliveira Neves LF, Camilo RP

    Model and system
    Critical review · No organism dosed
    Design
    Critical review of peptide use in sport and bodybuilding
    What was measured
    The 2026 review covered growth hormone secretagogues including ipamorelin, GHRH analogues and synthetic fragments promoted for muscle growth, fat metabolism and recovery.
    Reported findings
    The authors note these compounds are marketed as more selective and ostensibly safer alternatives to anabolic-androgenic steroids.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review; the promotional claims it describes are not endorsed by it.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • Model and system
    Narrative review · No organism dosed
    Design
    Narrative review of approved and unapproved peptides
    What was measured
    The 2026 review presented pharmacological mechanisms, safety profiles and regulatory status of approved and unapproved peptides marketed direct to patients.
    Reported findings
    The authors describe a parallel grey market of unapproved compounds operating largely outside regulatory oversight.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · Front Aging · Review or commentary · Grade R

    Therapeutic peptides in gerontology: mechanisms and applications for healthy aging

    Mavrych V, Shypilova I, Bolgova O

    Model and system
    Narrative review with searches of PubMed, Scopus and regulatory databases through January 2026 · No organism dosed
    Design
    Narrative review
    What was measured
    The 2026 review covered mechanisms, clinical applications, evidence base and safety profiles of therapeutic peptides with demonstrated or potential applications in healthy ageing.
    Reported findings
    Reported as a broad synthesis across peptide therapeutics in ageing.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review; anti-ageing framing is the authors’, and is not supported by primary ipamorelin research.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • Model and system
    Review of 106 articles across PubMed, ScienceDirect and SciELO · No organism dosed
    Design
    Narrative review prioritising systematic reviews, meta-analyses and randomised trials
    What was measured
    The 2026 review presented effects, clinical applications, safety profiles and regulatory status of prominent peptides, noting that novel unapproved compounds are expanding into preventive medicine and performance enhancement.
    Reported findings
    Reported as a synthesis across many peptides rather than an ipamorelin-specific appraisal.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · JBJS Rev · Review or commentary · Grade R

    Injectable Peptides in Sports Medicine: A Structured Narrative Review of Evidence, Safety, and Antidoping Implications

    Villegas Meza AD, Nocek M, Mitchell BC et al.

    Model and system
    Structured narrative review of PubMed/MEDLINE, Embase and Web of Science (Jan 2020 – Aug 2025) · No organism dosed
    Design
    Structured narrative review
    What was measured
    The 2026 review summarised human and translational evidence for injectable peptides relevant to orthopaedics and sports medicine, covering safety, product quality, regulatory and anti-doping implications.
    Reported findings
    The authors state that clinical adoption has outpaced high-quality evidence and regulatory consensus.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review; restricted date window; many compounds.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · Front Endocrinol (Lausanne) · Review or commentary · Grade R

    The emerging landscape of performance-enhancing peptides modulating GH-IGF1 axis: bridging the gap between clinical evidence and patient self-administration

    Dominikowski A, Rękoś Z, Olejarz M et al.

    Model and system
    Narrative review · No organism dosed
    Design
    Narrative review of GH-IGF-1 axis performance-enhancing compounds
    What was measured
    The 2026 review covered unregulated peptides marketed as research compounds that modulate the GH-IGF-1 axis, including ipamorelin among the growth hormone secretagogues.
    Reported findings
    The review addresses the gap between clinical evidence and patient selection for this compound class.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review spanning a whole compound class.

    Ipamorelin among several compounds tested · Growth hormone secretion, Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · Am J Sports Med · Review or commentary · Grade R

    Peptide Supplements and Their Therapeutic Applications in Sports Medicine

    Tewari K, Liu TP, Im C et al.

    Model and system
    Scoping review of PubMed by three independent reviewers · No organism dosed
    Design
    Scoping review
    What was measured
    The 2026 scoping review summarised peer-reviewed data on six peptides including ipamorelin for musculoskeletal recovery and enhancement.
    Reported findings
    The authors state these peptides are often perceived as low risk despite the absence of efficacy or safety data for many of them.
    Safety reporting
    Secondary source.
    Limitations
    Scoping review; covers six compounds, so its ipamorelin-specific content is limited.

    Ipamorelin among several compounds tested · Body composition, Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • 2026 · Sex Med Rev · Review or commentary · Grade R

    Peptides in urology and sexual medicine: clinical effectiveness, dosing, indications, and safety: a narrative review

    Vasylieva V, West A, Karpman E

    Model and system
    Structured narrative review of PubMed, Scopus and Google Scholar · No organism dosed
    Design
    Narrative review; 76 of 725 records met inclusion criteria
    What was measured
    The 2026 review covered mechanisms, clinical evidence, dosing, safety and regulatory status of peptide-based therapies in urology and sexual medicine, with ipamorelin among the growth hormone secretagogues searched.
    Reported findings
    The authors note that adoption is often influenced by off-label prescribing, direct-to-consumer promotion and limited long-term safety data.
    Safety reporting
    Secondary source.
    Limitations
    Narrative review covering many compounds; not an ipamorelin-specific evidence synthesis.

    Ipamorelin among several compounds tested · Safety reporting · Source verified 2026-11-11 · Editorial status: source verified

  • Model and system
    Tilapia (Oreochromis mossambicus), 21 days of dosing · Intraperitoneal
    Design
    Two-dose comparison against untreated control
    What was measured
    The study administered ipamorelin acetate at 5 or 30 µg for 21 days to tilapia and measured a dose-dependent rise in food intake alongside increased numbers of primary and secondary spermatocytes and early spermatids. GnRH-immunoreactive fibres did not differ between groups, while androgen receptor protein, serum LH and 11-ketotestosterone rose.
    Reported findings
    The authors proposed mediation through 11-ketotestosterone and androgen receptors at the testicular level and LH at the pituitary level.
    Safety reporting
    Not reported.
    Limitations
    A fish species with a reproductive endocrinology that does not map onto human physiology. Of interest for comparative endocrinology only.

    Ipamorelin itself · Reproduction · Source verified 2026-11-11 · Editorial status: source verified

  • Model and system
    Ferrets given cisplatin; isolated ferret ileum · Intraperitoneal
    Design
    Vehicle-controlled comparison of anamorelin and ipamorelin, with a separate intracerebroventricular arm for anamorelin
    What was measured
    The study measured whether ghrelin mimetics alleviated cisplatin-induced weight loss in ferrets. Ipamorelin inhibited electrical-field-stimulated ileal contractions by 54.4% (IC50 11.7 µM). Neither anamorelin nor ipamorelin given intraperitoneally affected acute or delayed emesis, but both reduced cisplatin-induced weight loss in the delayed phase (48–72 h) by approximately 24%.
    Reported findings
    Weight loss in the delayed phase was reduced; emesis was not.
    Safety reporting
    Not reported.
    Limitations
    Ferrets; a chemotherapy-toxicity model. The ileal concentrations are micromolar, far above receptor-level potencies.

    Ipamorelin among several compounds tested · Gastrointestinal motility, Body composition · Source verified 2026-11-11 · Editorial status: source verified

  • 2020 · Transl Androl Urol · Review or commentary · Grade R · Key record

    Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males

    Sinha DK, Balasubramanian A, Tatem AJ et al.

    Model and system
    Narrative review · No organism dosed
    Design
    Narrative review of growth hormone secretagogues in male hypogonadism
    What was measured
    The review examined the literature on growth hormone secretagogues including sermorelin, GHRP-2, GHRP-6, ibutamoren and ipamorelin as potential adjuncts in hypogonadism management.
    Reported findings
    The authors stated that current data on the clinical efficacy of these agents largely remain lacking, and that the paucity of data limits understanding of their role.
    Safety reporting
    Not a primary safety source.
    Limitations
    Narrative review. Its own conclusion is that clinical efficacy data are lacking; it is frequently cited as though it demonstrated benefit, which it does not.

    Ipamorelin among several compounds tested · Body composition · Source verified 2026-11-11 · Editorial status: source verified

  • 2020 · J Exp Pharmacol · Animal study (in vivo) · Grade C

    Attenuation of Visceral and Somatic Nociception by Ghrelin Mimetics

    N Mohammadi E, Louwies T, Pietra C et al.

    Model and system
    Rats with acetic-acid-induced visceral hypersensitivity without colonic inflammation · Intravenous
    Design
    Vehicle-controlled comparison of a peripherally restricted and a globally active ghrelin agonist, with receptor antagonist challenge
    What was measured
    The study measured visceral and somatic sensitivity in rats. Ipamorelin, described by the authors as peripherally restricted, and HM01 both reduced colonic hypersensitivity and somatic allodynia against vehicle controls, and both effects were blocked by the ghrelin receptor antagonist H0900.
    Reported findings
    The antagonist reversal supports a ghrelin-receptor-mediated mechanism for the observed change in nociceptive behaviour.
    Safety reporting
    Not reported.
    Limitations
    Rats; behavioural pain surrogates; no human data on this endpoint exists.

    Ipamorelin among several compounds tested · Nociception, Receptor pharmacology · Source verified 2026-11-11 · Editorial status: source verified

  • 2019 · Drug Test Anal · Analytical chemistry · Grade D · Key record

    Glycine-modified growth hormone secretagogues identified in seized doping material

    Gajda PM, Holm NB, Hoej LJ et al.

    Model and system
    Pharmaceutical preparations seized by Danish customs · No organism dosed
    Design
    Identification against reference standards by LC–HRMS
    What was measured
    The study analysed unknown preparations seized by Danish customs authorities and identified them as analogues of GHRP-2, GHRP-6, ipamorelin and modified GRF (1-29), in every case carrying an extra N-terminal glycine.
    Reported findings
    The authors concluded that analytical methods targeting growth hormone secretagogues should be updated to cover these glycine-extended forms.
    Safety reporting
    Not assessed. The finding concerns product identity, not toxicity.
    Limitations
    Seized samples; no information on prevalence or on the effects of the modified compounds.

    A modified form found in seized or market product · Product identity and quality, Analytical and anti-doping methods · Source verified 2026-11-11 · Editorial status: source verified

Every record, without JavaScript

The full table below carries the same records as the explorer above and renders on the server, so the data is available to readers and crawlers without scripting. How records are found, classified and graded is set out on the methodology page.

All 55 indexed ipamorelin records
StudyModel and routeWhat was measuredLimitationsGrade
Mayfield 2026
Am J Sports Med
Safety reporting
ReviewNo organism dosed
Narrative review
Among several
The 2026 review evaluated current evidence and applications of injectable peptide therapy in regenerative medicine and sports performance.Narrative review.Evidence grade R
Rahman 2026
J Am Acad Orthop Surg Glob Res Rev
Safety reporting
ReviewNo organism dosed
Narrative review
Among several
The 2026 review described signalling pathways attributed to therapeutic peptides and grouped ipamorelin with other secretagogues said to activate IGF-1 signalling and satellite cell repair.Narrative review. The mechanistic statements are broad and are not traceable to ipamorelin-specific primary studies within the review itself.Evidence grade R
Coutinho 2026
J Sports Med Phys Fitness
Safety reporting
ReviewNo organism dosed
Critical review
Among several
The 2026 review covered growth hormone secretagogues including ipamorelin, GHRH analogues and synthetic fragments promoted for muscle growth, fat metabolism and recovery.Narrative review; the promotional claims it describes are not endorsed by it.Evidence grade R
Mendias 2026
Sports Med
Safety reporting
ReviewNo organism dosed
Narrative review
Among several
The 2026 review presented pharmacological mechanisms, safety profiles and regulatory status of approved and unapproved peptides marketed direct to patients.Narrative review.Evidence grade R
Mavrych 2026
Front Aging
Safety reporting
ReviewNo organism dosed
Narrative review with searches of PubMed, Scopus and regulatory databases through January 2026
Among several
The 2026 review covered mechanisms, clinical applications, evidence base and safety profiles of therapeutic peptides with demonstrated or potential applications in healthy ageing.Narrative review; anti-ageing framing is the authors’, and is not supported by primary ipamorelin research.Evidence grade R
Renke 2026
Int J Mol Sci
Safety reporting
ReviewNo organism dosed
Review of 106 articles across PubMed, ScienceDirect and SciELO
Among several
The 2026 review presented effects, clinical applications, safety profiles and regulatory status of prominent peptides, noting that novel unapproved compounds are expanding into preventive medicine and performance enhancement.Narrative review.Evidence grade R
Villegas 2026
JBJS Rev
Safety reporting
ReviewNo organism dosed
Structured narrative review of PubMed/MEDLINE, Embase and Web of Science (Jan 2020 – Aug 2025)
Among several
The 2026 review summarised human and translational evidence for injectable peptides relevant to orthopaedics and sports medicine, covering safety, product quality, regulatory and anti-doping implications.Narrative review; restricted date window; many compounds.Evidence grade R
Dominikowski 2026
Front Endocrinol (Lausanne)
Growth hormone secretion · Safety reporting
ReviewNo organism dosed
Narrative review
Among several
The 2026 review covered unregulated peptides marketed as research compounds that modulate the GH-IGF-1 axis, including ipamorelin among the growth hormone secretagogues.Narrative review spanning a whole compound class.Evidence grade R
Tewari 2026
Am J Sports Med
Body composition · Safety reporting
ReviewNo organism dosed
Scoping review of PubMed by three independent reviewers
Among several
The 2026 scoping review summarised peer-reviewed data on six peptides including ipamorelin for musculoskeletal recovery and enhancement.Scoping review; covers six compounds, so its ipamorelin-specific content is limited.Evidence grade R
Vasylieva 2026
Sex Med Rev
Safety reporting
ReviewNo organism dosed
Structured narrative review of PubMed, Scopus and Google Scholar
Among several
The 2026 review covered mechanisms, clinical evidence, dosing, safety and regulatory status of peptide-based therapies in urology and sexual medicine, with ipamorelin among the growth hormone secretagogues searched.Narrative review covering many compounds; not an ipamorelin-specific evidence synthesis.Evidence grade R
Gouda 2024
Anim Reprod Sci
Reproduction
AnimalIntraperitoneal
Tilapia (Oreochromis mossambicus), 21 days of dosing
Ipamorelin itself
The study administered ipamorelin acetate at 5 or 30 µg for 21 days to tilapia and measured a dose-dependent rise in food intake alongside increased numbers of primary and secondary spermatocytes and early spermatids. GnRH-immunoreactive fibres did not differ between groups, while androgen receptor protein, serum LH and 11-ketotestosterone rose.A fish species with a reproductive endocrinology that does not map onto human physiology. Of interest for comparative endocrinology only.Evidence grade C
Lu 2024
Physiol Behav
Gastrointestinal motility · Body composition
AnimalIntraperitoneal
Ferrets given cisplatin; isolated ferret ileum
Among several
The study measured whether ghrelin mimetics alleviated cisplatin-induced weight loss in ferrets. Ipamorelin inhibited electrical-field-stimulated ileal contractions by 54.4% (IC50 11.7 µM). Neither anamorelin nor ipamorelin given intraperitoneally affected acute or delayed emesis, but both reduced cisplatin-induced weight loss in the delayed phase (48–72 h) by approximately 24%.Ferrets; a chemotherapy-toxicity model. The ileal concentrations are micromolar, far above receptor-level potencies.Evidence grade C
Sinha 2020
Transl Androl Urol
Body composition
ReviewNo organism dosed
Narrative review
Among several
The review examined the literature on growth hormone secretagogues including sermorelin, GHRP-2, GHRP-6, ibutamoren and ipamorelin as potential adjuncts in hypogonadism management.Narrative review. Its own conclusion is that clinical efficacy data are lacking; it is frequently cited as though it demonstrated benefit, which it does not.Evidence grade R
N 2020
J Exp Pharmacol
Nociception · Receptor pharmacology
AnimalIntravenous
Rats with acetic-acid-induced visceral hypersensitivity without colonic inflammation
Among several
The study measured visceral and somatic sensitivity in rats. Ipamorelin, described by the authors as peripherally restricted, and HM01 both reduced colonic hypersensitivity and somatic allodynia against vehicle controls, and both effects were blocked by the ghrelin receptor antagonist H0900.Rats; behavioural pain surrogates; no human data on this endpoint exists.Evidence grade C
Gajda 2019
Drug Test Anal
Product identity and quality · Analytical and anti-doping methods
AnalyticalNo organism dosed
Pharmaceutical preparations seized by Danish customs
Market product
The study analysed unknown preparations seized by Danish customs authorities and identified them as analogues of GHRP-2, GHRP-6, ipamorelin and modified GRF (1-29), in every case carrying an extra N-terminal glycine.Seized samples; no information on prevalence or on the effects of the modified compounds.Evidence grade D
Krug 2018
Growth Horm IGF Res
Product identity and quality · Analytical and anti-doping methods
AnalyticalNo organism dosed
Seized and market growth-promoting products
Market product
The study characterised products from the black market and identified three analogues of growth hormone releasing peptides as Gly-GHRP-6, Gly-GHRP-2 and Gly-Ipamorelin, each being the corresponding peptide extended by an N-terminal glycine residue. The identity of Gly-Ipamorelin was confirmed by custom synthesis.Analytical identification of seized material; the samples are not a representative survey of any market.Evidence grade D
Worm 2018
J Pept Sci
Receptor pharmacology
In vitroNo organism dosed
Ghrelin receptor activation assays
Analogue
The study generated boron-rich peptide conjugates targeting the ghrelin receptor and demonstrated the approach using the backbones of GHRP-6 and ipamorelin.Chemistry for a cancer-therapy delivery concept; no in vivo data and no relevance to ipamorelin itself.Evidence grade D
Fowkes 2018
Eur J Med Chem
Receptor pharmacology
In vitroNo organism dosed
Receptor binding and functional assays; radiochemistry
Analogue
The study prepared 4-fluorobenzoylated secretagogues derived from several scaffolds including ipamorelin to test positions for fluorine-18 insertion. The most suitable candidate was derived from G-7039, not ipamorelin, with IC50 69 nM and EC50 1.1 nM.The ipamorelin scaffold was among those screened but was not the selected compound.Evidence grade D
Ferro 2017
Drug Test Anal
Receptor pharmacology · Analytical and anti-doping methods
In vitroIntranasal
Radio-competitive binding assay at GHSR1a; urine from nasal-administration excretion studies
Among several
The study measured binding at the GHSR1a receptor for several growth hormone releasing peptides and truncated analogues sharing the core Ala-Trp-(D-Phe)-Lys, and confirmed receptor-assay activity in urine samples collected after nasal administration of GHRP-1, GHRP-2, GHRP-6, hexarelin and ipamorelin.Binding assay plus analytical application; no physiological outcome measured.Evidence grade D
Tsivou 2017
Drug Test Anal
Analytical and anti-doping methods
AnalyticalNo organism dosed
Urine in spray-coated collection containers, three WADA-accredited laboratories
Among several
The study tested a chemical stabilisation mixture spray-coated inside urine collection containers against enzymatic breakdown of proteins and small peptides including ipamorelin.Sample-handling research; no biological endpoint.Evidence grade D
Semenistaya 2016
Drug Test Anal
Analytical and anti-doping methods
AnalyticalNo organism dosed
Human urine
Among several
The study compared microelution-plate and cartridge solid-phase extraction, confirming effectiveness by analysis of urine samples containing ipamorelin, and found the microelution format raised limits of detection for 5 of 17 peptides.Analytical laboratory workflow only.Evidence grade D
Thomas 2016
J Sep Sci
Analytical and anti-doping methods
AnalyticalNo organism dosed
Human urine by direct injection
Among several
The study covered 17 prohibited peptides including ipamorelin with limits of detection between 50 and 500 pg/mL and identified −20 °C as the appropriate storage temperature for sports drug testing.Analytical; proof of concept used other peptides.Evidence grade D
Cox 2015
Drug Test Anal
Analytical and anti-doping methods
AnalyticalNo organism dosed
Urine samples from athletes
Among several
The study reported detection of GHRP-2 and GHRP-6 in urine samples from athletes. No abstract text is indexed for this record.No abstract is indexed in PubMed, so this entry rests on the title and journal alone. Ipamorelin is not named in the title; the record is retained because the search retrieved it within this method literature.Evidence grade D
Semenistaya 2015
Drug Test Anal
Pharmacokinetics · Analytical and anti-doping methods
HumanIntranasal
Healthy volunteers, single intranasal administration, urine collected for 2 days
Among severaln = One volunteer per compound
The study administered GHRP-1, GHRP-2, GHRP-6, hexarelin and ipamorelin intranasally, one volunteer each, and identified urinary metabolites. Hexarelin and ipamorelin were reported to metabolise intensively and to be excreted as parent compound together with metabolites; ipamorelin (1-4) free acid was detected in urine after the parent substance had cleared.One volunteer per compound, so this establishes that humans have received intranasal ipamorelin under study conditions but supports no conclusion about effect or safety. The purpose is anti-doping method development.Evidence grade B
Timms 2014
Drug Test Anal
Analytical and anti-doping methods
AnalyticalIntravenous
Equine and human urine; rat administration for proof of principle
Among several
The study presented a derivatisation method improving chromatography of basic peptides, detecting all eight growth hormone releasing peptides including ipamorelin, or their metabolites, in urine collected from rats after intravenous administration.Analytical; the administration component is in rats.Evidence grade D
Beck 2014
Int J Colorectal Dis
Gastrointestinal motility · Safety reporting
HumanIntravenous
Adults undergoing small and large bowel resection by open or laparoscopic surgery, 19 sites
Ipamorelin itselfn = 117 enrolled; 114 in the safety and modified intent-to-treat populations
The trial compared intravenous ipamorelin 0.03 mg/kg twice daily with placebo from postoperative day 1 to day 7 or hospital discharge. Median time to first tolerated meal was 25.3 hours with ipamorelin and 32.6 hours with placebo (P = 0.15). Any treatment-emergent adverse event occurred in 87.5% of the ipamorelin group and 94.8% of the placebo group.The authors describe the trial as small, with patients drawn from a broad range of underlying conditions. It is a proof-of-concept study in postoperative recovery; it was not designed to measure body composition, athletic recovery or ageing, and it reports no such endpoints.Evidence grade A
Kwok 2013
Anal Bioanal Chem
Analytical and anti-doping methods
AnalyticalNo organism dosed
Horse plasma
Among several
The study extracted seven peptides including ipamorelin from horse plasma with limits of detection below 50 pg/mL, and reported the first identification of in vitro metabolites of the studied peptides other than TB-500 in horses.Analytical; equine matrix.Evidence grade D
Thomas 2012
J Chromatogr A
Analytical and anti-doping methods
AnalyticalNo organism dosed
Human urine
Among several
The study developed a screening assay for 11 prohibited peptides including ipamorelin using weak cation exchange purification and nano-UHPLC with high-resolution tandem mass spectrometry, reporting recovery 45–95% and limits of detection 2–10 pg/mL.Analytical chemistry only; proof of principle used other peptides.Evidence grade D
Thomas 2012
Anal Chem
Analytical and anti-doping methods
AnalyticalOral
Rat in vivo administration; human serum and recombinant amidase in vitro
Among several
The study identified 28 metabolites, at least three for each of the growth hormone releasing peptides studied including ipamorelin, from rat in vivo samples, confirming the main ones in a human in vitro model. All arose from exopeptidase, amidase or endopeptidase activity.Analytical; the in vivo component is in rats.Evidence grade D
Greenwood-Van 2012
J Exp Pharmacol
Gastrointestinal motility
AnimalIntravenous
Fasted adult male rats after laparotomy and intestinal manipulation; isolated gastric fundus in organ bath
Ipamorelin itself
The study measured gastric emptying after abdominal surgery in rats. In vehicle controls 78% ± 5% of the meal remained in the stomach; after ipamorelin 0.014 µmol/kg intravenously, 52% ± 11% remained (P < 0.05), against 44% ± 6% in non-surgical controls. In isolated gastric smooth muscle, the surgery-induced inhibition of acetylcholine- and electrical-field-stimulated contractions was reversed by ipamorelin and by ghrelin.Rats; acute surgical model; ex vivo tissue for the mechanism component.Evidence grade C
Thomas 2011
Anal Bioanal Chem
Analytical and anti-doping methods
AnalyticalNo organism dosed
Human urine, spiked and from an excretion study
Among several
The study developed extraction and mass-spectrometric detection of eight growth hormone releasing peptides including ipamorelin from human urine, with recovery 47–95% and limits of detection 0.2–1 ng/mL.Analytical chemistry. It carries no information about effects in any organism.Evidence grade D
Aagaard 2009
Growth Horm IGF Res
Metabolism
AnimalSubcutaneous
Five groups of rats, seven days of dosing
Among several
The study measured hepatic alpha-amino-nitrogen conversion in prednisolone-treated rats. Prednisolone increased urea-N synthesis capacity and urea cycle gene expression and decreased nitrogen balance. Co-administered GH reduced urea-N synthesis capacity by 33% and improved nitrogen balance 2.5-fold; ipamorelin reduced it by 20% and neutralised nitrogen balance.Rats; the pair-fed control design is appropriate but the model is drug-induced catabolism, not ageing or athletic training.Evidence grade C
Venkova 2009
J Pharmacol Exp Ther
Gastrointestinal motility
AnimalIntravenous
Fasted male rats after laparotomy and intestinal manipulation
Ipamorelin itself
The study measured gastrointestinal transit in a rat model of postoperative ileus. A single dose of ipamorelin 1 mg/kg or GHRP-6 20 µg/kg shortened time to first bowel movement but did not change cumulative faecal output, food intake or body-weight gain at 48 h. Repeated dosing of ipamorelin at 0.1 or 1 mg/kg increased cumulative faecal pellet output, food intake and body-weight gain.Rats. The authors’ closing suggestion about patients is a hypothesis; the human trials that followed are indexed separately on this site.Evidence grade C
Yeung 2006
J Endocrinol
Receptor pharmacology
In vitroIntraperitoneal
Black seabream tissues, cDNA and genomic cloning, cell lines
Among several
The study cloned seabream ghrelin and examined its promoter; ghrelin expression was detected only in the stomach, and administration of growth hormone or ipamorelin to the fish in vivo enhanced that expression.Ipamorelin appears only as a tool compound in one experiment within a molecular-cloning paper on a fish species.Evidence grade D
Minamitake 2004
Nihon Rinsho
Receptor pharmacology
ReviewNo organism dosed
Narrative review in Japanese
Among several
A 2004 Japanese-language review of ghrelin structure–activity relationships. No abstract is indexed.Review; no abstract indexed; not in English.Evidence grade R
Shimatsu 2004
Nihon Rinsho
Growth hormone secretion
ReviewNo organism dosed
Narrative review in Japanese
Among several
A 2004 Japanese-language review of clinical perspectives on ghrelin-related drugs. No abstract is indexed.Review; no abstract indexed; not in English. Retained for completeness of the search, not used as evidence.Evidence grade R
Chan 2004
Comp Biochem Physiol C Toxicol Pharmacol
Growth hormone secretion · Receptor pharmacology
In vitroAdded to culture or bath
Primary culture of black seabream pituitary cells
Among several
The study measured GH release from seabream pituitary cells exposed to GHRP-2, ipamorelin, human ghrelin and two non-peptide secretagogues. All tested secretagogues except human ghrelin produced dose-dependent GH release with EC50 values in the nanomolar range, while GH mRNA levels did not change correspondingly even after 48 h.Fish cells in culture.Evidence grade D
Adeghate 2004
Neuro Endocrinol Lett
Metabolism
Ex vivoAdded to culture or bath
Pancreatic tissue fragments from normal and streptozotocin-diabetic rats
Ipamorelin itself
The study incubated pancreatic tissue fragments from normal and diabetic rats with ipamorelin at 10⁻¹² to 10⁻⁶ M. Ipamorelin increased insulin secretion from both (P < 0.04). Diltiazem, yohimbine, propranolol, or a combination of atropine, propranolol and yohimbine each significantly reduced this release; atropine alone reduced it in diabetic but not normal tissue.Excised tissue in a bath, not a living animal. Concentrations span six orders of magnitude. No human data exist on this endpoint.Evidence grade D
Johansen 2003
Exp Diabesity Res
Growth hormone secretion · Metabolism
AnimalIntravenous
Streptozotocin-diabetic and non-diabetic female mice, single intravenous injection
Ipamorelin itself
The study used ipamorelin as a provocation agent in streptozotocin-diabetic and non-diabetic mice. Ten minutes after injection, GH was 150 ± 35 µg/L in diabetic against 62 ± 11 µg/L in non-diabetic mice (P < .05). Serum IGF-I was lower in diabetic animals and rose after stimulation only in non-diabetic animals; hepatic IGF-I mRNA and peptide rose only in non-diabetic animals.Ipamorelin is the probe, not the subject. The study is useful mainly as evidence that a GH rise does not always produce an IGF-1 rise.Evidence grade C
Jiménez-Reina 2002
Histol Histopathol
Growth hormone secretion
AnimalSubcutaneous
Young female rats dosed for 21 days, then pituitary cell cultures
Ipamorelin itself
The study examined pituitary cells from young female rats given ipamorelin, GHRH or saline for 21 days. Somatotroph ultrastructure did not change but secretion granule volume density increased after ipamorelin or GHRH (P < 0.05). The percentage of somatotrophs and the ratio of strongly to weakly staining GH cells did not differ between groups at baseline in culture.Young female rats; histological and culture endpoints with no functional in vivo outcome.Evidence grade C
Peschke 2002
Eur J Med Chem
Receptor pharmacology
AnimalIntravenous
In vitro assay; swine
Analogue
Comparing ipamorelin with NN703 led the authors to add polar C-terminal groups to NN703; the resulting 4-hydroxypiperidino series showed low-nanomolar in vitro EC50 values and 40% oral bioavailability, with a GH Cmax above 40 ng/mL in a swine model.Ipamorelin appears only as the comparison point for analogue design.Evidence grade C
Lall 2001
Biochem Biophys Res Commun
Body composition · Metabolism
AnimalSubcutaneous
GH-deficient (lit/lit) and GH-intact mice, twice-daily subcutaneous dosing
Among several
The study compared ipamorelin and GH in GH-deficient and GH-intact mice. Ipamorelin produced a small (15%) body-weight increase by two weeks and increased fat pad weights relative to body weight in both lit/lit and +/lit mice; two weeks of ipamorelin or GHRP-6 increased relative body fat measured by DEXA in GH-intact mice. GH decreased relative fat mass in lit/lit mice. Secretagogue treatment, but not GH, increased serum leptin and food intake.Mice. The direction of the fat result is the opposite of what is commonly claimed for this compound class, and is reported here as the authors reported it.Evidence grade C
Ahnfelt-Rønne 2001
Endocrine
Receptor pharmacology · Growth hormone secretion
AnimalIntravenous
Rats, whole-body autoradiography and gastrointestinal resection
Analogue
The study found that NN703 and GHRP-6 accumulated in the glandular stomach of rats, and that resection of the gastrointestinal tract attenuated the GH response to GHRP-6 by 60–70% while leaving the GHRH response uninhibited.The compounds studied are NN703 and GHRP-6, not ipamorelin; ipamorelin appears in the derivation history only.Evidence grade C
Matsumoto 2001
Biochem Biophys Res Commun
Receptor pharmacology
In vitroAdded to culture or bath
Calcium mobilisation assay
Among several
The study explored structure–function relationships of the ghrelin N-terminus and noted that the resulting short analogues emerged structurally close to peptidyl growth hormone secretagogues.Ipamorelin is referenced as part of the compound class rather than tested as the subject.Evidence grade D
Hansen 2001
Bioorg Med Chem Lett
Receptor pharmacology
AnimalIntravenous
Rat pituitary cell assay; pigs
Analogue
The study prepared hybrids of NN703 and ipamorelin with lysine mimetics and naphthyl or biphenylalanine cores, and reported that re-introducing C-terminal pharmacophores produced compounds more potent than expected both in vitro and in pigs.Analogue chemistry; single-dose in vivo screening only.Evidence grade C
Andersen 2001
Growth Horm IGF Res
Bone · Body composition
AnimalSubcutaneous
Eight-month-old female rats, 3 months of subcutaneous injection
Ipamorelin itself
The study measured muscle strength and periosteal bone formation in rats given methylprednisolone 9 mg/kg/day, ipamorelin 100 µg/kg three times daily, or both for three months. In animals given the combination, maximum tetanic tension was significantly higher and periosteal bone formation rate four-fold higher than in animals given the glucocorticoid alone.The comparison is against glucocorticoid-treated rats, not against untreated animals; it is a counteraction of a drug-induced deficit in rats, not evidence of benefit in healthy subjects.Evidence grade C
Svensson 2000
J Endocrinol
Bone · Body composition
AnimalSubcutaneous
Thirteen-week-old female Sprague-Dawley rats, 12 weeks of continuous subcutaneous infusion
Among severaln = 7–8 per group
The study measured bone mineral content in rats given ipamorelin 0.5 mg/kg/day, GHRP-6 0.5 mg/kg/day, GH 3.5 mg/kg/day or vehicle for 12 weeks. All treatments increased body weight and total tibial and vertebral bone mineral content, but content corrected for body weight was unaffected, and total and vertebral areal bone mineral density were unchanged. Peripheral quantitative computed tomography showed the cortical increase came from greater cross-sectional bone area while cortical volumetric density was unchanged.Rats; female only. The result is explicitly one of bone dimensions, not density, and is the kind of distinction lost when summarised as "increases bone density".Evidence grade C
Johansen 1999
Growth Horm IGF Res
Bone · Growth hormone secretion
AnimalSubcutaneous
Adult female rats, 15 days of subcutaneous dosing three times daily
Ipamorelin itself
The study measured longitudinal growth rate in the proximal tibial metaphysis after 0, 18, 90 and 450 µg/day of ipamorelin for 15 days. Growth rate rose dose-dependently from 42 µm/day in the vehicle group to 44, 50 and 52 µm/day (P < 0.0001), with a dose-dependent increase in body-weight gain. Total IGF-I, IGF binding proteins and serum markers of bone formation and resorption were not changed by treatment.Rats; 15 days. The dissociation between bone growth and unchanged IGF-I limits inference about the GH–IGF-1 axis. No human equivalent exists.Evidence grade C
Hansen 1999
Eur J Endocrinol
Receptor pharmacology · Growth hormone secretion
AnimalOral
Rat pituitary cells; BHK cells expressing human GHS-R 1A; swine; beagle dogs; rats
Analogue
The study characterised NN703, an orally active secretagogue derived from ipamorelin. NN703 inhibited 35S-MK677 binding to the human GHS-R 1A, and in swine produced a 50% rise in cortisol over basal at all doses tested without dose-dependency. Oral bioavailability in dogs was 30% and a 14-day oral course increased body-weight gain in rats.The subject is NN703. Findings here must not be read across to ipamorelin, whose reported cortisol profile differs.Evidence grade C
Gobburu 1999
Pharm Res
Pharmacokinetics · Growth hormone secretion
HumanIntravenous
Healthy male volunteers, 15-minute intravenous infusions
Ipamorelin itselfn = 8 per dose level across 5 dose levels
The study measured pharmacokinetics and GH response after 15-minute infusions of 4.21, 14.02, 42.13, 84.27 and 140.45 nmol/kg. Pharmacokinetics were dose-proportional, with a terminal half-life of 2 hours, clearance of 0.078 L/h/kg and steady-state volume of distribution of 0.22 L/kg. GH release was a single episode peaking at 0.67 hours and declining exponentially to negligible concentrations at every dose. The concentration producing half-maximal GH stimulation was 214 nmol/L.Healthy young men only; single infusions; the measured endpoint is hormone concentration, not any clinical outcome. PubMed indexes this record with the publication types "Clinical Trial" and "Randomized Controlled Trial", but the published abstract describes a dose-escalation design and does not describe randomisation or a placebo control, so it is graded here as a human study without a control group.Evidence grade B
Malmlöf 1999
Growth Horm IGF Res
Growth hormone secretion · Body composition
AnimalIntravenous
Rats given methylprednisolone, with venous catheters, 10 days of intravenous dosing four times daily
Ipamorelin itself
The study measured whether methylprednisolone blunted the GH response to ipamorelin in rats. The acute plasma GH response to ipamorelin or GHRH was unchanged by glucocorticoid. Over 10 days, glucocorticoid-treated rats lost 13.6 ± 2.9 g against 4.0 ± 3.5 g in saline controls, while rats given glucocorticoid plus ipamorelin lost 2.3 ± 2.0 g (high dose) and 1.6 ± 2.0 g (low dose); IGF-I rose in parallel.Rats recovering from surgery and receiving a glucocorticoid; not a healthy-animal model.Evidence grade C
Ankersen 1998
J Med Chem
Receptor pharmacology · Pharmacokinetics
AnimalIntravenous
Rat pituitary cell assay; anaesthetised rats; swine; dogs
Analogue
The study described a series of secretagogues derived from the ipamorelin scaffold by size reduction and backbone N-methylation. The tetrapeptide NNC 26-0235 showed an ED50 of 2 nmol/kg in swine and 10% oral bioavailability in dogs; the report notes that NNC 26-0235 and ipamorelin each raised basal GH more than ten-fold after oral doses of 1.8 and 2.7 mg/kg respectively.The subject is the analogue series, not ipamorelin. Oral doses given were very large relative to intravenous ED50 values.Evidence grade C
Hansen 1998
J Med Chem
Receptor pharmacology
AnimalIntravenous
Rat pituitary assay; swine; dogs
Analogue
The study reduced the size of the lead compound ipamorelin and introduced backbone isosteres, reporting oral bioavailability of 10–55% for most tested compounds and an in vivo ED50 of 30 nmol/kg in swine for the most potent.Describes analogues rather than ipamorelin itself.Evidence grade C
Raun 1998
Eur J Endocrinol
Growth hormone secretion · Receptor pharmacology
AnimalIntravenous
Primary rat pituitary cells; pentobarbital-anaesthetised rats; conscious swine
Ipamorelin itself
This 1998 report described the discovery of ipamorelin as a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) and measured GH release from primary rat pituitary cells (EC50 1.3 ± 0.4 nmol/l, Emax 85 ± 5% of GHRP-6), in anaesthetised rats (ED50 80 ± 42 nmol/kg) and in conscious swine (ED50 2.3 ± 0.03 nmol/kg). Antagonist profiling indicated GH release through a GHRP-like receptor rather than the GHRH receptor. In swine, none of the secretagogues tested altered FSH, LH, PRL or TSH; GHRP-6 and GHRP-2 raised ACTH and cortisol, whereas ipamorelin did not raise them significantly above levels seen after GHRH stimulation, at doses more than 200-fold above its GH ED50.Animal and cell models only. The selectivity finding is a measurement of pituitary hormone levels in swine after acute dosing, not a human safety result. Conducted by the originator company.Evidence grade C
Johansen 1998
Xenobiotica
Pharmacokinetics
AnimalIntranasal
Male rats, intravenous and intranasal dosing
Among several
The study compared the pharmacokinetics of ipamorelin, NNC 26-0194, NNC 26-0235, GHRP-2 and GHRP-6 in male rats. After intravenous bolus, plasma concentrations declined biexponentially; ipamorelin showed a systemic plasma clearance five-fold lower than GHRP-6 and was excreted mainly in urine, whereas GHRP-6 was excreted predominantly in bile. Nasal bioavailability of ipamorelin was estimated at approximately 20%, against roughly 50% for the three comparators.Rat pharmacokinetics do not transfer to humans. Nasal bioavailability was estimated, not measured against an absolute intravenous reference in the same animals.Evidence grade C

References

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  2. Gobburu JV, Agersø H, Jusko WJ et al. (1999). Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. Pharm Res. PubMed 10496658 · doi:10.1023/a:1018955126402[Human, grade B]
  3. Raun K, Hansen BS, Johansen NL et al. (1998). Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. PubMed 9849822 · doi:10.1530/eje.0.1390552[Animal, grade C]