Ipamorelin is a peptide that is 5 amino acids in length, comprised of both proteinogenic and non-proteinogenic amino acids in this sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2
Ipamorelin was originally developed by Novo Nordisk A/S, a multinational pharmaceutical company headquartered in Denmark, as a first-in-class selective growth hormone secretagogue (ie. a substance which promotes the secretion of GH) . Subsequently, it licensed to Helsinn Therapeutics for a phase II clinical trial for the treatment of postoperative ileus, a complication that can manifest after abdominal surgery . Although this trial demonstrated that ipamorelin was ineffective for mitigating the symptoms of ileus, it nevertheless demonstrated an excellent safety profile in humans, which is crucial information when considering other potential uses of ipamorelin, such as athletic performance enhancement. Currently Ipamorelin is being investigated for the potential to improve a variety of age-associated problems in the following ways:
In preclinical and clinical studies, Ipamorelin has been administered subcutaneously to maximize serum levels. However, due to its small size and favorable pharmacokinetics, it also shows decent bioavailability after absorption via sublingual (under the tongue) or intranasal administration, albeit with slightly less efficiency .
In clinical trials, Ipamorelin is being evaluated at 50-300 micrograms/day.
Selected clinical research findings
Ipamorelin administration increases natural growth hormone (GH) production in healthy humans :
Forty-eight healthy, non-smoking, male subjects with a mean age of 31 years (range: 25-41 years) and a mean weight of 77 kg (range: 59-100 kg) were enrolled in the trial. Subjects with insulin-like growth factor-1 (IGF-1) concentrations out of normal range, history of drug sensitivity, allergy, or any subjects who were otherwise unsuitable were not included in the study. The trial was performed in accordance with the Declaration of Helsinki and approved by the local Ethics Committee. This trial was a randomized, placebo-controlled dose-escalation study in which five groups received a 15 minute infusion of ipamorelin or a placebo. Blood samples were obtained after dosing to determine the plasma ipamorelin and GH concentrations.
Adapted from: J. V. S. Gobburu, H. Agersø, W. J. Jusko, and L. Ynddal, “Pharmacokinetic-Pharmacodynamic Modeling of Ipamorelin, a Growth Hormone Releasing Peptide, in Human Volunteers,” Pharm. Res., vol. 16, no. 9, pp. 1412–1416, 1999.
Increased natural growth hormone (GH) production in increases cognitive function in healthy adults :
It has been suggested that the declines in growth hormone (GH) and insulin-like growth factor I (IGF-I) observed with advancing age may contribute to the impaired cognitive function associated with aging and perhaps to that seen in neurodegenerative diseases such as Alzheimer's disease. GH and IGF-I are present in the plasma and the cerebrospinal fluid, and both have binding sites in the CNS, including in the choroid plexus and particularly in the hippocampus, a brain structure crucial to learning and memory. Significant negative correlations have been observed between advancing age and the density of GH binding sites, especially in the pituitary, hypothalamus and hippocampus. Cognitive deficits are also seen in GH-deficient adults and can be normalized by GH therapy…Here we report the results of a prospective, randomized, placebo-controlled, double-blinded study of the effects of 6 months of [GH-increasing] treatment on the cognitive function of healthy older men and women.
Adapted from: M. V. Vitiello, K. E. Moe, G. R. Merriam, G. Mazzoni, D. H. Buchner, and R. S. Schwartz, “Growth hormone releasing hormone improves the cognition of healthy older adults,” Neurobiol. Aging, vol. 27, no. 2, pp. 318–323, Feb. 2006.
Conclusions: These studies provide clear evidence that Ipamorelin increases GH levels in humans, and increased GH levels improve the cognitive function of healthy older men and women on a number of cognitive tasks. Six months of GH-increasing treatment resulted in significant improvement in cognitive functions, particularly those that involve problem solving and psychomotor processing speed (e.g., WAIS-R PIQ, WAIS-R PA, SDT, FINDA) and working memory (LETSET) of both healthy older men and women.
Selected preclinical research findings
Ipamorelin increases bone mineral content to strengthen bones :
Growth hormone (GH) is of importance for normal bone remodeling. The aim of the present study was to investigate whether theipamorelin (IPA) and GH-releasing peptide-6 (GHRP-6), increasebone mineral content (BMC)in young adult rats. Thirteen-week-old female Sprague–Dawley rats were given IPA (05 mg/kg per day; n=7), GHRP-6 (05 mg/kg per day; n=8), GH (35 mg/kg per day; n=7), or vehicle administered subcutaneously for 12 weeks. The animals were followed in vivo by dual X-ray absorptiometry (DXA) measurements every 4th week. After the animals were killed, femurs were analyzed in vitro by mid-diaphyseal peripheral quantitative computed tomography (pQCT) scans. All treatments increased body weight and total tibial and vertebral BMC measured by X-ray in vivo compared with vehicle-treated controls. However, total BMC corrected for the increase in body weight (total BMC:body weight ratio) was unaffected. Tibial area bone mineral density (BMD, BMC/area) was increased, but total and vertebral area BMDs were unchanged. The pQCT measurements in vitro revealed that the increase in the cortical BMC was due to an increased cross-sectional bone area, whereas the cortical volumetric BMD was unchanged. We conclude that treatment of adult rats with ipamorelin or GHRP-6 increases BMC as measured by X-ray in vivo.
IPA = Ipamorelin; BMC = bone mineral content Adapted from: J. Svensson et al., “The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats,” J. Endocrinol., vol. 165, no. 3, pp. 569–577, Jun. 2000.
*The information herein is for educational and informational purposes only. THIS PRODUCT IS FOR RESEARCH USE ONLY. For use in animal studies, all research must be conducted with oversight from the appropriate Institutional Animal Care and Use Committee (IACUC) following the guidelines of the Animal Welfare Act (AWA).
Storage: Lyophilized peptide should be stored at -20°C (freezer), and the reconstituted peptide solution at 4°C (refrigerated). Use within 24 months. Once reconstituted use within 30 days. Do not freeze once reconstituted.
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 J. V. S. Gobburu, H. Agersø, W. J. Jusko, and L. Ynddal, “Pharmacokinetic-Pharmacodynamic Modeling of Ipamorelin, a Growth Hormone Releasing Peptide, in Human Volunteers,” Pharm. Res., vol. 16, no. 9, pp. 1412–1416, 1999.
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 P. B. Johansen et al., “Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats,” Growth Horm. IGF Res., vol. 9, no. 2, pp. 106–113, May 1999.
 J. Svensson et al., “The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats,” J. Endocrinol., vol. 165, no. 3, pp. 569–577, Jun. 2000.
 L. D. Baker et al., “Effects of Growth Hormone–Releasing Hormone on Cognitive Function in Adults With Mild Cognitive Impairment and Healthy Older Adults,” Arch. Neurol., vol. 69, no. 11, p. 1420, Nov. 2012.
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 M. V. Vitiello, K. E. Moe, G. R. Merriam, G. Mazzoni, D. H. Buchner, and R. S. Schwartz, “Growth hormone releasing hormone improves the cognition of healthy older adults,” Neurobiol. Aging, vol. 27, no. 2, pp. 318–323, Feb. 2006.
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