Ipamorelin
clinical trialsAlso 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
C38H49N9O5Research & studies
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.
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.
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.
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.
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.
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.
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.
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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