Ipamorelin

clinical trials

Also known as: NNC 26-0161

Ipamorelin (NNC 26-0161) is a synthetic pentapeptide that acts as a selective agonist at the growth hormone secretagogue receptor (GHS-R1a), mimicking the action of ghrelin. Its mechanism involves binding to GHS-R1a in the pituitary and hypothalamus, leading to a pulsatile release of growth hormone (GH) without significantly elevating cortisol or prolactin levels. This selectivity distinguishes it from earlier GHS-R agonists and reduces off-target endocrine effects. Key research findings from clinical trials indicate that ipamorelin enhances GH secretion in a dose-dependent manner, with a favorable safety profile. Studies have demonstrated its potential to increase lean body mass and improve gastrointestinal motility in postoperative ileus, while showing no significant impact on insulin-like growth factor 1 (IGF-1) levels at therapeutic doses. Its short half-life and oral bioavailability in preclinical models have supported further investigation into its pharmacokinetics and tolerability. Clinically, ipamorelin has been explored for conditions such as GH deficiency, frailty in aging, and postoperative recovery, though it remains in clinical trial phases. Its minimal effect on other pituitary hormones reduces the risk of hyperprolactinemia or hypercortisolism, making it a candidate for targeted GH modulation. However, long-term safety and efficacy data are still under evaluation. For research purposes only — not medical advice.

Key data

Category
Growth Hormone Peptides
Molecular weight
711.9 g/mol
Molecular formula
C38H49N9O5
CAS number
170851-70-4
Half-life
~2 hours
Administration
subcutaneous
Research status
clinical trials
References
49
Tags
ghrp, ghrelin-mimetic, selective

Research & studies

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
Physiology & behavior · 2024 · PubMed

Intraperitoneal anamorelin and ipamorelin reduced cisplatin-induced weight loss by ~24% during the delayed phase (48-72 h).; Neither compound affected acute or delayed emesis when given intraperitoneally.; Intracerebroventricular anamorelin reduced acute emesis by 60% and improved food/water intake by 20-40% during the acute phase.; Both compounds inhibited electrical field stimulation-induced contractions of isolated ferret ileum.

Attenuation of Visceral and Somatic Nociception by Ghrelin Mimetics
Journal of experimental pharmacology · 2020 · PubMed

Ghrelin mimetics HM01 and ipamorelin reduced colonic hypersensitivity and somatic allodynia in rats without active inflammation.; The anti-nociceptive effects were reversed by the ghrelin receptor antagonist H0900.; A peripherally restricted ghrelin mimetic (ipamorelin) was effective in attenuating both visceral and somatic pain.; Ghrelin receptor-mediated mechanisms are involved in non-inflammatory visceral and somatic hypersensitivity.

Analysis of new growth promoting black market products
Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society · 2018 · PubMed

A modified GH with an additional N-terminal alanine (192 amino acids, 22,195 Da) was discovered and confirmed via top-down and bottom-up mass spectrometry.; Three new GHRP analogues (Gly-GHRP-6, Gly-GHRP-2, Gly-Ipamorelin) were identified, each extended by an N-terminal glycine residue.; Custom synthesis and high-resolution tandem mass spectrometry confirmed the structures of Gly-Ipamorelin and Gly-GHRP-2.; In-vitro experiments provided preliminary data on the potential metabolism of these peptides after administration.

Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients
International journal of colorectal disease · 2014 · PubMed

Ipamorelin 0.03 mg/kg twice daily for up to 7 days was well tolerated with 87.5% adverse event rate vs 94.8% for placebo.; Median time to first tolerated solid meal was 25.3 hours for ipamorelin vs 32.6 hours for placebo (p=0.15).; No significant differences were observed in key or secondary efficacy analyses.; The study was small and enrolled patients with a broad range of underlying conditions.

Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats
Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society · 2009 · PubMed

Prednisolone increased hepatic urea-N synthesis capacity (CUNS) and urea cycle gene expression while decreasing nitrogen balance and organ nitrogen contents.; Co-administration of GH reduced CUNS by 33%, normalized urea cycle gene expression, and improved nitrogen balance 2.5-fold.; Ipamorelin reduced CUNS by 20%, decreased urea cycle enzyme expression, and neutralized nitrogen balance.; Both GH and Ipamorelin counteracted steroid-induced nitrogen wasting, but GH was more efficient at the given doses.

Influence of chronic treatment with the growth hormone secretagogue Ipamorelin, in young female rats: somatotroph response in vitro
Histology and histopathology · 2002 · PubMed

Chronic Ipamorelin or GHRH treatment increased the volume density of secretion granules in somatotroph cells.; Basal intracellular GH content was lower in both Ipamorelin and GHRH groups compared to saline.; Only in the Ipamorelin group did acute treatment with Ipamorelin, GHRP-6, or GHRH increase the percentage of somatotroph cells.; Ipamorelin uniquely enhanced intracellular GH content in response to acute secretagogue stimulation.

The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats
Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research Society · 2001 · PubMed

Ipamorelin counteracted glucocorticoid-induced decrease in bone formation in adult rats.; Combined treatment increased periosteal bone formation rate four-fold versus glucocorticoid alone.; Maximum tetanic tension of calf muscles was significantly increased with combined treatment.; The growth hormone secretagogue reversed both muscle strength and bone formation declines caused by glucocorticoids.

Growth hormone (GH)-independent stimulation of adiposity by GH secretagogues
Biochemical and biophysical research communications · 2001 · PubMed

Ipamorelin increased body weight by 15% in both GH-deficient and GH-intact mice within 2 weeks.; GHS treatment increased fat pad weights relative to body weight in both mouse groups.; GH decreased relative fat mass in GH-deficient mice but had no effect in GH-intact mice.; GHS, but not GH, increased serum leptin and food intake in GH-intact mice.

Frequently asked questions

What is Ipamorelin?

Ipamorelin (NNC 26-0161) is a synthetic pentapeptide that acts as a selective agonist at the growth hormone secretagogue receptor (GHS-R1a), mimicking the action of ghrelin. Its mechanism involves binding to GHS-R1a in the pituitary and hypothalamus, leading to a pulsatile release of growth hormone (GH) without signifi

How does Ipamorelin work?

Selective ghrelin receptor (GHS-R1a) agonist that stimulates GH release with minimal effect on cortisol or prolactin.

What is the research status of Ipamorelin?

Ipamorelin is currently classified as clinical trials, with 49 research references on record. This is for research purposes only and is not medical advice.

What is the half-life of Ipamorelin?

The reported half-life of Ipamorelin is ~2 hours.

What is the molecular weight of Ipamorelin?

Ipamorelin has a molecular weight of approximately 711.9 g/mol (formula C38H49N9O5).

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