Ipamorelin

What Is Ipamorelin?

Ipamorelin represents a short peptide sequence with binding capability to the ghrelin/growth hormone secretagogue receptor. Among the most selective growth hormone (GH) secretagogues identified, it has demonstrated in laboratory studies its effects on ACTH, prolactin, follicle-stimulating hormone, luteinizing hormone, thyroid-stimulating hormone, and cortisol release. Ghrelin possesses high specificity levels, making ipamorelin valuable for research purposes both as a therapeutic agent and as a model peptide for comprehending selectivity mechanisms in ghrelin receptor activation.

Ipamorelin Research

1. Ipamorelin and Negative Corticosteroid Effects

Glucocorticoids, the class of corticosteroids frequently employed to address inflammation in conditions spanning cancer to autoimmune disease, carry a range of serious side effects that commonly restrict their therapeutic utility. Reducing the adverse effects of glucocorticoids could enable higher medication dosages—and potentially milder side effects—to remain active for extended durations, both of which might yield positive outcomes for morbidity and mortality. Ipamorelin has demonstrated in animal studies its capacity to mitigate the adverse effects of glucocorticoid administration.

2. Ipamorelin and Bone Health

Among the most significant problems linked to extended glucocorticoid administration is decreased bone density and heightened fracture risk. Present therapeutic approaches include bisphosphonates, hormone therapies, and new functional antibodies. While these treatments prove effective individually, they all carry side effects, demonstrate limited efficacy, or incur high costs. Ipamorelin, conversely, offers the potential to completely reverse these effects through a highly restricted range of side effects. Rat studies reveal that ipamorelin can fully prevent bone loss attributable to corticosteroid administration and may even stimulate bone formation in rats subjected to these medications. Additional research demonstrates that ipamorelin also enhances bone mineral density substantially, thereby improving strength and potentially lowering fracture risk. In animal models, ipamorelin helps mitigate various other side effects of steroids. These additional effects extend beyond bone to internal organ disposition.

3. Ipamorelin and Muscle Growth

Evidence suggests that GH and growth hormone secretagogues such as ipamorelin may diminish the catabolic effects that glucocorticoids exert on muscle tissue. Rat research given glucocorticoids demonstrates a reduction in nitrogen wasting in the liver and a decrease in nitrogen balance after ipamorelin administration. Muscle wasting constitutes one of the most prevalent side effects linked to glucocorticoid use and represents a frequent treatment complication. Studies indicate that combining ipamorelin with a single dose might prove highly advantageous for patients requiring glucocorticoid therapy.

4. Ipamorelin and Diabetes

Diabetic rat research has shown that ipamorelin can facilitate insulin release. This effect is particularly beneficial during periods of reduced stimulation of pancreatic beta cells where insulin production and storage occur. Ipamorelin's effects on the pancreas involve better long-term functional capacity of pancreatic islets and contribute to developing novel therapeutic or preventative measures.

5. Studies for Treatment of Post-Operative Ileus

Post-operative ileus represents a condition that develops following certain surgical procedures, particularly common after abdominal surgery. The condition manifests as an inability of intestines to contract adequately because the GI system remains in a dormant state. This can be identified by pain, though the primary concern with POI involves sluggish discharge from hospital and extended recovery periods.

Ipamorelin has undergone investigation in multiple proof-of-concept clinical studies to assess whether peptide administration can reduce POI. Research indicates that ipamorelin does facilitate motility restoration within 12 hours following administration. Unfortunately, these studies revealed that ipamorelin's effectiveness proved insufficient to establish it as a commercially viable product. Hope exists that continuing research can improve efficacy, or that research may identify synergistic effects when combined with other compounds that will make the peptide more therapeutically useful.

6. Ipamorelin as Ghrelin Receptor Probe

Ipamorelin functions as a selective ghrelin receptor agonist and demonstrates strong binding affinity to the ghrelin receptor. This receptor plays a significant role in increasing abundance of cancer cells (such as human carcinomas) and heart failure. Given these characteristics, researchers have recognized that ipamorelin could serve as a probe for tumors, such as for diagnosis using techniques like positron emission tomography (PET) scanning. In vitro research has established the viability of this methodology and has validated that ipamorelin effectively labels tumors, which is necessary to detect such malignancies. The subsequent phase involves employing the probe to evaluate how effectively it aids in establishing standards for PET studies, particularly with interpreting PET studies associated with cancer.

Ipamorelin Is Neglected in Research

While ipamorelin lacks orphan drug designation at present, it remains a neglected focus in research environments. Despite relatively limited early studies, interest in ipamorelin has grown significantly in recent years following the determination not to develop it as a treatment for post-operative ileus. Ipamorelin demonstrates interest in numerous disease conditions along with their physiologic effects.

Ipamorelin shows moderate side effects, low oral and excellent subcutaneous bioavailability in mice. Dosage scaling in mice does not translate directly to humans. Ipamorelin from Peptide Sciences is restricted to educational and scientific research purposes only, but for licensed researchers, ipamorelin offers access if you are a licensed researcher.

1. Stomach residual food quantity remains lower in rats administered POI following ipamorelin administration, even when compared to rats not experiencing POI.
2. The geometric positioning of food shows similarity to rats without POI when rats with POI receive ipamorelin.
3. Redistribution of food location exhibits greater distal positioning in GI tract, resembling rats without POI, following ipamorelin administration.

Article Author

The above content was researched, edited, and organized by Dr. Logan, M.D. Dr. Logan possesses a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Scientific Journal Author

David E. Beck, MD, co-author of "Prospective, randomized, controlled, proof of concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients" specializes in colon and rectal surgery.

David E. Beck, MD is being referenced as one of the leading scientists involved in the research and development of ipamorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Peptide Sciences and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development work conducted by the scientists studying this peptide. David E. Beck, MD is listed in [6] under the referenced citations.

Referenced Citations

1. K. Raun et al., "Ipamorelin, the first selective growth hormone secretagogue," Eur. J. Endocrinol., vol. 139, no. 5, pp. 552–561, Nov. 1998. [PubMed]
2. N. B. Andersen, K. Malmlöf, P. B. Johansen, T. T. Andreassen, G. Ørtoft, and H. Oxlund, "The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decreases 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]
3. 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]
4. N. K. Aasgaard 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]
5. E. Adegoke and A. S. Ponrny, "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]
6. 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]
7. 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]
8. M. M. Fowkes, T. Lalonde, L. Yu, S. Dhanvantari, M. S. Kovacs, and L. G. Luyt, "Peptidominetic growth hormone secretagogue derivatives for positron emission tomography imaging of the ghrelin receptor," Eur. J. Med. Chem., vol. 157, pp. 1506–1511, Sep. 2018. [Science Direct]