Compound Overview
Class of Compound
Peptide
Mechanism of Action:
As an analogue of growth hormone-releasing hormone, sermorelin binds to the growth hormone-releasing hormone receptor of the anterior pituitary gland, thus stimulating the secretion of growth hormone.
Also Known As:
Geref, Gerel, sermorelin acetate, 114466-38-5, UNII-00IBG87IQW
Research Applications:
- GH regulation
- Muscle growth and recovery
- Anti-aging
Risks:
- Lack of long-term data
- No longer FDA approved
- Banned by WADA
Chemical Structure
What is Sermorelin?
Sermorelin is a synthetic peptide analogue of human growth hormone-releasing hormone (GHRH). It was developed by the German firm EMD Serono for the treatment of growth hormone deficiency (GHD) in both children and adults. The peptide’s primary function is to stimulate the manufacture and release of growth hormone (GH) in the human body.
Following clinical trials, sermorelin was initially approved by the U.S. Food and Drug Administration (FDA) in 1997 and sold under the trade name “Geref,” indicated for the treatment of growth hormone deficiency (GHD) in both children and adults [1, 2]. Its FDA approval was discontinued in 2008 for commercial reasons unrelated to its safety or efficacy [3].
Sermorelin was also used as a diagnostic agent for assessing whether a given patient’s pituitary gland was functioning properly and releasing adequate amounts of GH [1, 2].
The peptide is now being researched for applications beyond the diagnosis and treatment of hormone deficiency, including for its role in sleep quality, heart health, and even as a novel brain tumor treatment.
What Does Sermorelin Do?
Sermorelin contains the first 29 amino acids of growth hormone-releasing hormone and is the shortest synthetic peptide to offer the full biological activity of endogenous GHRH [4].
As an analog of GHRH, sermorelin also binds to the growth hormone-releasing hormone receptor found in the anterior pituitary gland, signaling to the pituitary gland to produce and release more growth hormone in the body, by way of somatotropic cells.
Sermorelin’s mechanism is different from that of biosynthetic hGH, since injection of the latter can raise GH in the body to supraphysiological levels. On the other hand, the primary function of sermorelin is to mimic native GRF and stimulate GH secretion to the maximum natural level. [4].
Sermorelin Benefits | Clinical Trials
Our team conducted a literature review using PubMed, Google Scholar, and EMBASE to identify the relevant benefits and uses of sermorelin. Here are three of the most notable:
Effective treatment of adult-onset growth hormone insufficiency: Sermorelin is an effective and attractive treatment of adult-onset GH insufficiency. Unlike rhGH, sermorelin does not stimulate IGF-1 production in the liver and instead stimulates the pituitary gland to produce and secrete endogenous hGH, giving it a number of clinical advantages over exogenous hGH.
Notably, according to a 2006 article by Richard Walker, overdoses of endogenous hGH are “difficult if not impossible to achieve” as the effects of sermorelin are regulated by negative feedback involving the inhibitory neurohormone, somatostatin.
Sermorelin is not associated with the pro-cancer and pro-diabetes side effects linked to long-term hGH therapy, and is thus heavily researched to treat adult-onset GH insufficiency along with being used in longevity medicine for preserving youthful anatomy and physiology [5].
Positive effects on body composition: Sermorelin has been identified as one of several growth hormone secretagogues (GHS) that can help manage body composition in hypogonadal males. In a 2020 paper, Deepankar et al. noted that sermorelin can “significantly improve body composition” (in hypogonadal males) while “ameliorating specific hypogonadal symptoms” such as fat gain and muscular atrophy [6].
While the authors suggest that sermorelin could be used to achieve lean mass gain in both hypogonadal males and men with subclinical hypogonadism, to date, there is no published research that has investigated sermorelin’s effect on body composition in healthy subjects, highlighting an area for further research.
Potential anti-aging benefits: A 1992 study identified sermorelin’s potential anti-aging benefits after nine young male test subjects (22 to 33 years old) and ten elderly male test subjects (60 to 78 years old) were administered the peptide. The study found that short-term subcutaneous sermorelin injections enabled healthy male test subjects to reverse age-related decreases in GH and levels of IGF-I [7].
A 1997 single-blind randomized placebo-controlled trial found that elderly male and female test subjects who received nightly subcutaneous injections of sermorelin for 16 weeks experienced a “significant increase in skin thickness.” The peptide was found to produce significant increases in lean body mass in male test subjects and notable increases in libido and wellbeing. Male test subjects gained an average of 1.26 kg of lean body mass by the end of the trial [8]
Sermorelin and heart health: Sermorelin has been investigated alongside other GHRH agonists as a potential treatment for myocardial infarction scarring in swine [9]. The 2015 study found that sermorelin offered a number of benefits in post-heart attack animal models, which included:
- Reduced remodeling following a heart attack
- Increased growth of blood vessels in damaged tissue
- Reduction in cell death in cardiomyocytes
As a result, there is research interest in sermorelin’s heart health-related benefits, namely in its potential to treat problems resulting from cardiac remodeling and ability to heal damage in myocytes following a heart attack.
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Sermorelin Side Effects
According to a review of sermorelin’s use in the diagnosis and treatment of children with GHD, once daily subcutaneous doses of the peptide were well tolerated [4]. The review noted that the most commonly reported adverse events were transient facial flushing and injection site pain.
According to Drugs.com, the most common sermorelin side effects are [10]:
- Facial flushing
- Headache
- Nausea
- Pain
- Redness, or swelling at injection site
- Paleness
- Strange taste in mouth
- Vomiting
Is Sermorelin Safe?
Sermorelin currently lacks FDA approval as its approval was withdrawn in 2008 for reasons other than safety and efficacy [3]. Data on the safety of sermorelin for non-medical uses such as improving body composition in healthy subjects remains lacking.
As noted by Prakash and Goa, while sermorelin is a “well-tolerated” GHRH analogue when used as a provocative test of GHD in children, such tests would involve a single intravenous 1 μg/kg body weight dose and tell us very little about the peptide’s long-term safety [4].
According to Walker, sermorelin is potentially safer than exogenous rhGH because it does not stimulate IGF-1 and is virtually incapable of causing overdose, given that the peptide merely stimulates endogenous hGH and its effects are regulated by somatostatin [5].
Sermorelin Dosage Calculator
Research suggests that sermorelin is commonly administered at doses starting from 100-200 mcg per day for objectives like improved body composition, often in combination with other growth hormone secretagogues such as ipamorelin.
When used in longevity research, sermorelin is typically cycled for three to six months.
In terms of timing, Prakash and Goa’s research indicates that in the diagnosis and treatment of GH deficiency in children, it was common to administer sermorelin at night before bed, at least two hours after eating, or first thing in the morning when endogenous GH levels are typically at their peak.
Where to Buy Sermorelin Online? | 2024 Edition
Researchers looking to source high-quality sermorelin online should turn to our top recommended vendor:
Xcel Peptides
Xcel Peptides is a US-based vendor that offers research-grade sermorelin in 5mg vials for $40 per unit.
We fully endorse this vendor for the following reasons:
- Quality Assurance: Xcel Peptides has a rigorous quality control program in place to ensure that all of its peptides are up to standard. They source their peptides from cGMP approved manufacturers.
- Fast Shipping: Xcel Peptides offers fast shipping for free on domestic orders over $200. Orders generally arrive in 2-5 business days.
- High-Quality Information: The vendor’s website includes detailed research summaries of each peptide up for sale, as well as articles on how to properly handle peptides and more.
To obtain high-quality sermorelin and other peptides, head directly to Xcel Peptides.
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FAQ
Sermorelin | Reviews
Sermorelin has an array of both proven and potential benefits and uses, and may be used to improve body composition, achieve anti-aging benefits, and promote heart health.
The peptide has been approved by the FDA, and is backed by extensive literature that establishes it as an attractive alternative to hGH therapy.
To purchase sermorelin online, we recommend the vendor with the purest peptides and most secure buying experience online.
References
- Xu, Z. (2016). Growth Hormone-Releasing Hormone. In Handbook of Hormones (pp. 144-e18B). Academic Press.
- US Food and Drug Administration, (n.d.). Drugs at FDA: FDA-Approved drugs. https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=020443
- Determination That GEREF (Sermorelin Acetate) Injection, 0.5 Milligrams Base/Vial and 1.0 Milligrams Base/Vial, and GEREF (Sermorelin Acetate) Injection, 0.05 Milligrams Base/Amp, Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness. (2021). Retrieved 3 June 2021, from https://www.federalregister.gov/documents/2013/03/04/2013-04827/determination-that-geref-sermorelin-acetate-injection-05-milligrams-basevial-and-10-milligrams
- Prakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs. 1999 Aug;12(2):139-57. doi: 10.2165/00063030-199912020-00007. PMID: 18031173.
- Walker RF. Sermorelin: a better approach to management of adult-onset growth hormone insufficiency? Clin Interv Aging. 2006;1(4):307-8. doi: 10.2147/ciia.2006.1.4.307. PMID: 18046908; PMCID: PMC2699646.
- Sinha, Deepankar K et al. “Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males.” Translational andrology and urology vol. 9,Suppl 2 (2020): S149-S159. doi:10.21037/tau.2019.11.30
- Corpas E, Harman SM, Piñeyro MA, Roberson R, Blackman MR. Growth hormone (GH)-releasing hormone-(1-29) twice daily reverses the decreased GH and insulin-like growth factor-I levels in old men. J Clin Endocrinol Metab. 1992 Aug;75(2):530-5. doi: 10.1210/jcem.75.2.1379256. PMID: 1379256.
- Khorram O, Laughlin GA, Yen SS. Endocrine and metabolic effects of long-term administration of [Nle27]growth hormone-releasing hormone-(1-29)-NH2 in age-advanced men and women. J Clin Endocrinol Metab. 1997 May;82(5):1472-9. doi: 10.1210/jcem.82.5.3943. PMID: 9141536.
- Bagno, L. L., Kanashiro‐Takeuchi, R. M., Suncion, V. Y., Golpanian, S., Karantalis, V., Wolf, A., … & Valdes, D. (2015). Growth hormone–releasing hormone agonists reduce myocardial infarct scar in swine with subacute ischemic cardiomyopathy. Journal of the American Heart Association, 4(4), e001464.
- Drugs.com (2015). Sermorelin acetate. https://www.drugs.com/cdi/sermorelin-acetate.html
- World Anti-Doping Agency. World Anti-Doping Code International Standard Prohibited List 2022. WADA website. January 1, 2022. Accessed Mar 2022. https://www.wada-ama.org/sites/default/files/resources/files/2022list_final_en.pdf
- Baumann, G. P. (2012). Growth hormone doping in sports: a critical review of use and detection strategies. Endocrine Reviews, 33(2), 155-186.
- Laron, Z. (1995). Growth hormone secretagogues. Drugs, 50(4), 595-601.
- Ishida, J., Saitoh, M., Ebner, N., Springer, J., Anker, S. D., and von Haehling, S. (2020) Growth hormone secretagogues: history, mechanism of action, and clinical development. JCSM Rapid Communications, 3: 25– 37. https://doi.org/10.1002/rco2.9.
- Chang Y, Huang R, Zhai Y, Huang L, Feng Y, Wang D, Chai R, Zhang W, Hu H. A potentially effective drug for patients with recurrent glioma: sermorelin. Ann Transl Med 2021;9(5):406. doi: 10.21037/atm-20-6561.