Other names ：Ipamorelin [INN], UNII-Y9M3S784Z6, Y9M3S784Z6, NNC-260161
Ipamorelin, a synthetic peptide of the growth hormone-releasing peptide class, which has some potential benefits, including weight loss, greater lean muscle mass, better sleep, collagen formation, cellular repair, and IGF-1 stimulation. Ipamorelin also improves bone mineral content, mitigates the effects of glucocorticoids, and regulates appetite without producing excessive hunger. It distinguishes itself from conventional medications by controlling appetite and gastrointestinal motility without causing hunger and avoiding considerable cortisol increase.
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Ipamorelin [INN], UNII-Y9M3S784Z6, Y9M3S784Z6
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Beck DE, Sweeney WB, McCarter MD (December 2014). “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. 29 (12): 1527–34.
Moulin A, Ryan J, Martinez J, Fehrentz JA (September 2007). “Recent developments in ghrelin receptor ligands”. ChemMedChem. 2 (9): 1242–59.
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Gobburu JV, Agersø H, Jusko WJ, Ynddal L (September 1999). “Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers”. Pharmaceutical Research. 16 (9): 1412–6.
Jiménez-Reina L, Cañete R, De la Torre MJ, Bernal G (2002). “Chronic In Vivo Ipamorelin Treatment Stimulates Body Weight Gain and Growth Hormone (GH) Release In Vitro in Young Female Rats”. European Journal of Anatomy. 6 (1): 37–46.
Andersen NB, Malmlöf K, Johansen PB. The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. Growth Horm IGF Res. 2001 Oct;11(5):266-72.
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iustina A, Veldhuis JD. Pathophysiology of the neuroregulation of growth hormone secretion in experimental animals and the human. Endocrine Reviews. 1998;19(6):717–797.
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Russell-Aulet M, Jaffe CA, Demott-Friberg R, Barkan AL. In vivo semiquantification of hypothalamic Growth hormone-releasing hormone (GHRH) output in humans: Evidence for relative GHRH deficiency in aging. J Clin Endocrinol Metab. 1999;84:3490
Devesa, J., Almengló, C., & Devesa, P. (2016). Multiple Effects of Growth Hormone in the Body: Is it Really the Hormone for Growth?. Clinical medicine insights. Endocrinology and diabetes, 9, 47–71.
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Roy G. Smith, Development of Growth hormone Secretagogues, Endocrine Reviews, Volume 26, Issue 3, 1 May 2005, Pages 346–360.
What Is Ipamorelin?
Ipamorelin is a short peptide sequence that exhibits the ability to bind to the ghrelin/growth hormone secretagogue receptor. Among the known growth hormone (GH) secretagogues, it is one of the most selective ones. Laboratory studies have demonstrated that ipamorelin does not have any effect on the release of ACTH, prolactin, follicle-stimulating hormone, luteinizing hormone, thyroid-stimulating hormone, or cortisol. Its remarkable specificity has made it a subject of interest in research, both as a potential therapeutic agent and as a model peptide for studying the mechanisms of receptor binding selectivity.
Peptide Sequence: Aib-His-D-2Nal-D-Phe-Lys
Molecular Formula: C38H49N9O5
Molecular Weight: 711.868 g/mol
PubChem CID: 9831659
CAS Number: 170851-70-4 .
1. Ipamorelin and Negative Corticosteroid Effects
Glucocorticoids, a type of corticosteroids commonly employed in the treatment of inflammation associated with conditions ranging from cancer to autoimmune diseases, are known to have significant side effects that often restrict their efficacy. Alleviating these side effects could potentially enable higher dosing of glucocorticoids and prolong their usage, which could lead to positive outcomes in terms of morbidity and mortality. Several studies have demonstrated that ipamorelin can effectively diminish or even reverse the adverse effects associated with glucocorticoid administration.
2. Ipamorelin and Bone Health
One of the most significant challenges associated with long-term use of glucocorticoids is the loss of bone density and the subsequent risk of fractures. Current treatment options include bisphosphonates, hormone therapies, and new monoclonal antibodies. While these therapies are effective in their own ways, they also come with side effects, limited efficacy, or high costs. In contrast, ipamorelin is relatively inexpensive to produce and has minimal side effects. Studies conducted on rats have shown that ipamorelin can completely halt bone loss caused by corticosteroids and even lead to a four-fold increase in bone formation in rats exposed to these drugs. Furthermore, additional research indicates that ipamorelin improves systemic bone mineral density, thereby enhancing the strength of both existing and newly formed bones. As an added benefit, ipamorelin helps counteract some of the other side effects of steroids, such as muscle wasting and increased accumulation of visceral fat.
3. Ipamorelin and Muscle Growth
Evidence suggests that growth hormone (GH) and growth hormone secretagogues, such as ipamorelin, may help reduce the catabolic effects of glucocorticoids on muscle. Studies conducted on rats treated with glucocorticoids have shown a decrease in nitrogen wasting in the liver and an improved nitrogen balance after ipamorelin administration. Muscle wasting is a significant side effect associated with glucocorticoid use and often limits the effectiveness of treatment. Having a single drug that can counteract both muscle catabolism and bone density loss could provide substantial benefits to patients who require glucocorticoid therapy.
4. Ipamorelin and Diabetes
Research conducted on diabetic rats has discovered that ipamorelin has the ability to enhance insulin release. This effect is believed to occur through the indirect stimulation of the calcium channel present in pancreatic islet cells, which are responsible for the production and storage of insulin. By studying ipamorelin’s impact on the pancreas, we can gain insights into the functional constraints of type 2 diabetes and potentially develop new therapeutic approaches or preventive strategies.
5. Studied for Treatment of Post-Operative Ileus
Post-operative ileus (POI) is a frequent occurrence that often follows specific surgical procedures, with abdominal surgery being particularly susceptible to this condition. It manifests as an impaired gastrointestinal (GI) system, rendering individuals unable to consume oral nutrition. Symptoms may include pain, but the main issue with POI is its impact on hospital discharge rates and overall recovery duration, as it hampers the normal passage of bowel movements.
Ipamorelin has undergone several proof-of-concept clinical trials aimed at evaluating its potential in reducing post-operative ileus (POI). The research indicates that ipamorelin can shorten the time to the first meal by approximately 12 hours. However, despite initial promising results, the trials were discontinued as the conducting company determined that the efficacy of ipamorelin alone was not sufficient to develop a viable product. Nevertheless, there is optimism that ongoing research efforts can enhance its efficacy or that combination therapies incorporating ipamorelin may yield a synergistic effect with other compounds, ultimately leading to a more effective treatment option.
- The amount of radiolabeled food remaining in the stomach is lower in rats with POI after administration of ipamorelin, even when compared to rats without POI.
- The spatial distribution of the food is similar to that of rats without POI when ipamorelin is given to rats with POI.
- The location of radiolabeled food in the gastrointestinal (GI) tract becomes more distal and similar to that of rats without POI after the administration of ipamorelin.
6. Ipamorelin as Ghrelin Receptor Probe
Ipamorelin, a selective ghrelin receptor agonist, exhibits strong binding affinity to the ghrelin receptor. The expression of the ghrelin receptor is known to increase in certain cancer types, such as human carcinomas, as well as in heart failure. Based on these findings, researchers have recently hypothesized that ipamorelin could serve as a probe in positron emission tomography (PET) to aid in diagnosis. Preliminary in vitro studies have shown the feasibility of this approach and have confirmed that ipamorelin, which can be easily synthesized in a laboratory, could potentially be utilized as a PET probe. The next crucial step involves testing the probe in vivo to assess its functionality and establish standards for interpreting PET studies conducted with it.
Ipamorelin Is Neglected in Research
While ipamorelin does not currently hold orphan drug status, it remains an underexplored drug in research settings. Despite promising initial studies, the interest in ipamorelin has diminished following the decision to discontinue its development as a treatment for post-operative ileus. However, ipamorelin possesses numerous potential benefits, not only as a therapeutic agent but also as a valuable tool for enhancing our understanding of various disease states and their physiological impacts. It is likely that ipamorelin will regain research interest once new data and innovative insights into the advantages of this distinctive peptide emerge, reigniting the field. 
Ipamorelin demonstrates moderate side effects, low oral bioavailability, and excellent subcutaneous bioavailability in mice. However, the dosage per kilogram in mice cannot be directly extrapolated to humans. It is important to note that Ipamorelin available for purchase at Peptide Sciences is strictly intended for educational and scientific research purposes, and is not suitable for human consumption. Therefore, only licensed researchers should consider purchasing Ipamorelin.
 K. Raun et al., “Ipamorelin, the first selective growth hormone secretagogue,” Eur. J. Endocrinol., vol. 139, no. 5, pp. 552–561, Nov. 1998. [PubMed]
 N. B. Andersen, K. Malmlöf, P. B. Johansen, T. T. Andreassen, G. Ørtoft, and H. Oxlund, “The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats,” Growth Horm. IGF Res. Off. J. Growth Horm. Res. Soc. Int. IGF Res. Soc., vol. 11, no. 5, pp. 266–272, Oct. 2001. [PubMed]
 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. [ [PubMed]
 N. K. Aagaard et al., “Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats,” Growth Horm. IGF Res. Off. J. Growth Horm. Res. Soc. Int. IGF Res. Soc., vol. 19, no. 5, pp. 426–431, Oct. 2009. [PubMed]
 E. Adeghate and A. S. Ponery, “Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats,” Neuro Endocrinol. Lett., vol. 25, no. 6, pp. 403–406, Dec. 2004. [PubMed]
 D. E. Beck, W. B. Sweeney, M. D. McCarter, and Ipamorelin 201 Study Group, “Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients,” Int. J. Colorectal Dis., vol. 29, no. 12, pp. 1527–1534, Dec. 2014. [PubMed]
 B. Greenwood-Van Meerveld, K. Tyler, E. Mohammadi, and C. Pietra, “Efficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus,” J. Exp. Pharmacol., vol. 4, pp. 149–155, Oct. 2012. [PubMed]
Scientific Journal paper Author:
Health Care Chemistry, Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark
2.Peter B. Johansen
Department of Pharmacological Research, Novo Nordisk A/S, Bagsværd, DK-2880, Denmark
Department of Connective Tissue Biology, Institute of Anatomy, University of Aarhus, Aarhus C, DK-8000, Denmark
4.Niels Kristian Aagaard
Department of Medicine V (Hepatology and Gastroenterology), Aarhus University Hospital, DK-8000 Aarhus C, Denmark
Center for Preventive Doping Research and Institute of Biochemistry, German Sport University Cologne, Germany
Institute of Biochemistry/Center for Preventive Doping Research, German Sport University Cologne, Am Sportpark Müngersdorf, 50933 Cologne, Germany