Outlook Spotlight

Sermorelin Peptide Therapy | A-Z Guide

Curious about Sermorelin peptide therapy? Inside, we detail everything you need to know about the research chemical – dosing, benefits, side effects, and more.

Sermorelin Peptide Therapy
info_icon

This in-depth guide on Sermorelin peptide therapy was crafted by the research team at Peptides.org– the premier source for all information about research peptides, SARMs, and more.

Sermorelin is a synthetic peptide derived from an endogenous hormone called growth hormone-releasing hormone (GHRH). Similar to GHRH, sermorelin exerts its effects in the pituitary gland by binding to somatotroph cells leading to secretion of growth hormone.

The peptide was previously approved by the United States Food and Drug Administration (FDA) for treatment of short stature disorder, proving to be safe and effective at inducing catch-up growth in undersized children through increasing GH and insulin-like growth factor 1 (IGF-1). 

Similarly, human trials have demonstrated that sermorelin can safely increase GH and IGF-1 levels in healthy older adults, leading to fat loss and increased lean body mass. 

Sermorelin and related GH-releasing peptides are the subject of research interest based on claims that they can deliver several highly sought-after anti-aging effects associated with increased GH such as improved body composition, thicker skin, improved well-being, and libido. 

For qualified researchers looking to buy research-grade sermorelin peptide, the team at Peptides.org recommends using the industry leader Peptide Sciences.

What is Sermorelin?

Sermorelin, originally referred to as GHRH (1-29), is a 29 amino acid peptide derived from the first 29 amino acids of the endogenous peptide hormone, growth hormone-releasing hormone (GHRH) [1]. 

Sermorelin falls into a category of compounds called growth hormone secretagogues (GHSs), defined by the ability to increase the natural production of growth hormone (GH) [2].

Within the family of GHSs, there are two subcategories:

•    Compounds that bind to the growth hormone secretagogue receptor (GHS-R), which is the receptor for ghrelin; and,
•    Compounds that bind to the growth hormone-releasing hormone receptor (GHRHR), which is the receptor for endogenous GHRH.

Sermorelin falls into the second category of GHSs that bind to GHRH, which is not surprising as it is an identical 29-amino acid fragment derived from GHRH. 

Sermorelin first received FDA approval in 1990 for diagnosis of GH deficiency. This is due to the peptide’s ability to rapidly increase GH secretion, making it a useful diagnostic tool for determining the cause of growth deficiencies in children [2]. 

Further evaluation of sermorelin in children led to a second FDA approval in 1997 for treatment of children with growth failure due to idiopathic GH deficiency, as it was shown to increase GH release and growth velocity in children during a 36-month study [3].

Despite demonstrated efficacy, sermorelin was withdrawn in 2008 by its manufacturer EMD Serono due to manufacturing issues and poor sales, as it was out-competed by recombinant human growth hormone (rhGH), which proved to be more effective in treating children with growth deficiencies [2, 4]. 

Interestingly, the same reason for the mild effects in children is why sermorelin may be a better option for adults looking to treat low levels of GH and IGF-1, for reasons that will be described in more detail below. 

info_icon
Sermorelin

What Does Sermorelin Do?

Sermorelin is a 29-amino acid peptide derivative of the endogenous peptide hormone GHRH, that retains the full functional activity of GHRH, due to the fact that the sermorelin peptide includes the GHRH receptor binding domain [2].

Advertisement

Sermorelin has a rapid half life of 11-12 minutes when administered via injection and exerts its effects by binding to the GHRH receptor at the pituitary gland [2]. This leads to stimulation of growth hormone secretion by the pituitary gland, independent of changes to other hormones such as luteinizing hormone (LH), follicle-stimulating hormone (FHS), prolactin, cortisol, glucose, glucagon, or thyroid stimulating hormone (TSH) [5, 6].

Unlike administration of GH which introduces an unnatural, single bolus of the hormone, sermorelin leads to stimulation of pulsatile GH secretion that mirrors endogenous secretion patterns [7]. It is hypothesized that GH secretion in this pulsatile fashion over a 24-hour period is important for reaping the full benefits of the GH-IGF-1 axis [8].

An important byproduct of sermorelin’s targeting of the underlying regulatory feedback pathway is that GH and IGF-1 levels are maintained in a physiological range, avoiding the negative consequences of GH therapy [9]. 

Similar to hGH administration, the most notable effects of sermorelin are around increased lipolysis due to direct action of GH on adipose tissue and increased lean body mass due to upregulation of IGF-1 secretion [2, 10]. 

Due to these unique properties, sermorelin is useful to researchers interested in an alternative to exogenous rhGH administration that can produce the following effects, all otherwise associated with rhGH [7]:

•    Diagnosis of growth hormone deficiency
•    Treatment of low IGF-1 levels
•    Improvements in body composition and fat loss
•    Improved muscle strength and exercise performance
•    Increased skin thickness
•    Improved memory and well-being
•    Increased resting energy expenditure

Advertisement

Sermorelin Clinical Trials and Research 

Sermorelin has been evaluated across numerous human trials for a variety of reasons related to the induction of growth hormone and IGF-1 secretion. Noteworthy results will be highlighted in this section. 

Diagnosis of growth hormone deficiency

Several studies have demonstrated that sermorelin is effective for the diagnosis of growth hormone deficiency (GHD), leading to FDA approval in 1990 [2]. Sermorelin is useful for this application as it is capable of potently and rapidly inducing growth hormone secretion in subjects with an intact hypothalamic-pituitary axis (HPA), allowing clinicians to understand the origin of the growth hormone deficiency [4, 10].

Treatment of short stature in children

Sermorelin received an additional FDA approval for the treatment of children with short stature in 1997. It was shown to effectively induce catch-up growth in 74% of growth hormone deficient children after six months of treatment. Sermorelin was well-tolerated in this population when administered once per day via subcutaneous injection at a dose of 30mcg/kg prior to bedtime [3, 5].

Increased growth hormone secretion in healthy adults

In an 1985 study evaluating various analogues of GHRH, intravenous (IV) administration of sermorelin (referred to as GHRH(1-29)-NH2) was shown to lead to an increase in plasma growth hormone levels, with similar potency to endogenous GHRH. Notably, sermorelin was well-tolerated and did not affect levels of other hormones controlled by the pituitary [6].

Several follow-up studies confirmed that sermorelin can induce increased growth hormone secretion, even in the elderly who have lower endogenous levels of growth hormone [11].

Advertisement

Further studies have confirmed that once or twice-daily subcutaneous injections of sermorelin are capable of elevating IGF-1 levels in elderly men. This is a critical finding since IGF-1 is responsible for mediating many of the desirable effects of GH [1, 12].

Two different longer-term studies evaluating once-daily subcutaneous injection of sermorelin in older men and women demonstrated several benefits of sermorelin treatment [10]:

•    Roughly 2x secretion of GH
•    Increased IGF-1 levels
•    Increased lean body mass and reduced fat

In a 2017 study that examined the synergistic effects of sermorelin along with the growth hormone secretagogues GHRP-2 and GHRP-6 in hypogonadal men on testosterone replacement therapy, 100mcg of each compound was administered three times per day via subcutaneous injection [9].

The combination of growth hormone-stimulating peptides led to a statistically significant increase in IGF-1 levels in all men without any changes to LH, FSH, or E levels. Interestingly, statistically significant increases in testosterone were also observed at the first follow-up window and maintained throughout the duration of the study [9]. 

Improvement in cognitive function

Sermorelin has been shown to have positive effects on cognitive function due to upregulation of IGF-1. Following six months of daily treatment with sermorelin, older adults showed a statistically significant improvement in several measures of IQ [13]. 

Follow-up studies using additional GHRH analogs found similar results, prompting significant attention on the role of the GH-IGF-1 axis in treating age-related conditions like Alzheimer’s disease [14].

info_icon
Sermorelin

Sermorelin Safety and Side Effects

Across several clinical trials in children and adults, sermorelin was found to be an exceptionally safe compound, with the only reported side effects related to minor injection-site irritation [2]. 

Advertisement

Part of the reason that sermorelin has such an excellent safety profile is that it leverages the built-in safety circuits that exist to keep GH and IGF-1 levels in a physiological range [2, 4]. 

This is because sermorelin has an identical peptide sequence to the first 29 amino acids of the endogenous GHRH and binds to the same receptor in the anterior pituitary gland, leading to growth hormone release. As a result, downstream GH secretion leverages the natural secretion pathways and all of the associated regulatory mechanisms that ensure GH remains in range.

Specifically, GH is subject to negative feedback inhibition, such that GH secretion is inhibited if GH levels go above a certain threshold [4, 8]. This natural regulatory mechanism also ensures that IGF-1 levels are kept within a natural range, which is important for safety because excess IGF-1 leads to many of the unwanted effects that have been observed with rhGH therapy [7]. 

As noted by a subject-matter expert interviewed to understand the safety of the peptide, sermorelin’s ability to leverage natural GH regulatory pathways and feedback inhibition makes it very difficult to overdose since downstream GH production is capped [15]. Nonetheless, a rational sermorelin dosing protocol is advised and will be covered below.

Despite the well-established safety profile, researchers are still encouraged to use biomarkers to understand sermorelin’s effects in different test populations. Most importantly, IGF-1 levels should be monitored, as it is more stable with a longer half-life than GH and therefore a more useful readout of GH secretion [2, 7]. 

Although human trials did not find that sermorelin peptide therapy led to the hyperglycemia and insulin resistance associated with rhGH, researchers may be interested in monitoring glucose and insulin sensitivity if patients are diabetic or pre-diabetic [10].

In summary, sermorelin is well-tolerated with the most common side effects related to injection site-reactions. 

Is Sermorelin Legal? 

Although sermorelin was previously FDA approved, it is no longer available as a medical product as its production was discontinued by the manufacturer. Note that this was not due to issues around safety or efficacy, but for commercial reasons, as noted above. 

Like many other research peptides, sermorelin is available for purchase, sale, and handling for research purposes and not as a medical product.

Sermorelin’s current classification prevents it from being marketed in the United States for human consumption and for the treatment of medical conditions. Sermorelin is similarly classified in the United Kingdom and in the European Union. 

The gap in regulatory oversight for peptides like sermorelin has led to the emergence of an unregulated peptide market with unqualified and unauthorized vendors inappropriately marketing products with unsupported medical claims.

These vendors are subject to legal penalties in several countries including the US and the UK, while consumers bear the health risks of administering adulterated compounds. 

Current Peptide Regulations

Given the nascent stage of peptide therapies like sermorelin, the regulatory framework is lacking, even within the legal peptide market. This presents a challenging environment for the approval of peptide products to be evaluated in clinical trials and eventually distributed as medical goods. 

Despite the ambiguity around regulations, there is massive demand for peptide products in the United States and many countries globally, with growth rates pointing to even higher demand in the future. 

As noted above, qualified researchers are advised to be aware of vendor quality and exercise caution around purchasing decisions. Vendors with long track-records of delivering high-quality, research-grade peptides should be prioritized. 

Sermorelin for Competitive Athletics

For researchers intending to apply their work towards competitive sport, it is important to note that sermorelin is classified as a banned substance by multiple doping agencies due to its potential for enhancing athletic performance. 

It is specifically treated as a class S2 non-specified substance by the World Anti-Doping Agency (WAD), a classification that has also been adopted by the United States Anti-Doping Agency (USADA) [15, 16].

Sermorelin Dosage and Cycle

Sermorelin has been administered at a relatively wide range of doses in various human clinical trials via both intravenous (IV) and subcutaneous (sc) injection [10]. In this section, we summarize the current thinking around dosing of sermorelin by experts in the field.

As we have noted, sermorelin’s mechanism of action leverages the natural GH secretion pathway with resulting GH levels maintained within a physiological range by the natural regulatory machinery [2]. 

As a result, the peptide  is unique in that increasing sermorelin dosages above a certain level does not result in increased effects on GH and IGF-1 [4, 17]. Nonetheless, we recommend that researchers use a conservative dosing protocol and use the minimal therapeutic dose. 

A hypothetical dosing protocol to help researchers understand how sermorelin might be dosed in a potential trial is as follows:

•    Tolerance assessment: To assess tolerance, begin with a dose of 100mcg injected subcutaneously. (Note that 1mg is equal to 1000mcg, and 100mcg is equal to 1/10th of a milligram)

•    Low-dose protocol (200mcg/day): Since sermorelin has a short half-life, administer 100mcg via sc injection in the morning and again in the evening before bed, for a total of 200mcg. 

•    High-dose protocol (600mcg/day): For users who do not respond to the low dose protocol, administer 200mcg of sermorelin in the morning, afternoon, and prior to bedtime for a total of 600mcg.

The most useful biomarker for understanding whether sermorelin is having an effect at a given dosage is IGF-1. Therefore, to best assess the effects of a particular dose of sermorelin, we recommend that researchers get baseline blood work with follow-up bloodwork after at least 2 weeks at a given dosing protocol. 

Based on the available literature, sermorelin does not appear to require cycling and has been administered in trials for up to 36 months of continuous usage. 

Note that sermorelin peptide will be lyophilized into a freeze-dried powder after manufacturing to improve temperature stability and increase shelf life. Prior to injection, researchers will need to use bacteriostatic water to reconstitute and dissolve the freeze-dried peptide into an injectable liquid solution. 

info_icon
Sermorelin

Where to Buy Sermorelin Online? 

Qualified researchers interested in studying sermorelin in preclinical laboratory testing may be interested to find out the best place to buy sermorelin online. 

Our review team at Peptides.org has experience with several online vendors and has determined that the best source for injectable sermorelin peptide is: 

Peptide Sciences has an unparalleled reputation within the research peptide space and meets all of our criteria for identifying the highest quality peptide sources:

•    Quality and Purity. Peptide Sciences produces research-grade sermorelin using manufacturing processes that are subject to rigorous quality control standards, ensuring that researchers can generate results unaffected by impurities. 

•    Excellent Pricing. Peptide Sciences offers competitive pricing alongside top-notch quality and customer service. A 5mg sermorelin vial currently retails for $49.50 and bulk pricing is available for large orders. 

•    Multiple Payment Methods. Peptide Sciences accepts Cash App, Zelle, Bitcoin, Ether, as well as e-check. The vendor keeps your payment information and data secure with SSL encryption.

•    Customer Service. Peptide Sciences has a reputable customer service department and has a dedicated team that can handle questions or concerns about orders. 

How to Reconstitute Sermorelin

Upon receipt of shipment, sermorelin will arrive as a lyophilized powder in a glass vial. Lyophilization preserves the biological activity of the peptide in a temperature-stable format, allowing shipment and extended shelf life. 

To prepare sermorelin for injection, researchers will need to reconstitute the lyophilized peptide with bacteriostatic water. This will dissolve the powder into a clear liquid that can be drawn up into a syringe.

Prior to reconstitution, ensure that a sufficient amount of bacteriostatic water is available. Note that bacteriostatic water is recommended for reconstitution, as it will protect the peptide against contamination for at least 1 month due to the presence of 0.9% benzyl alcohol.

Bacteriostatic water, along with other supplies needed for injection of sermorelin, can be purchased from BacteriostaticWater.org. 

Once bacteriostatic water is on hand, determine the volume needed to dilute the peptide to the desired concentration. Refer to the following protocol for instructions on how to complete reconstitution:

•    Clean hands and swab the rubber stopper on the sermorelin vial, as well as the bacteriostatic water vial.

•    Insert the needle into the bacteriostatic water vial and draw up the required volume of water.

•    Remove the syringe and insert it into the sermorelin vial, ensuring that the full volume of bacteriostatic water is dispensed prior to removal.

•    Gently rotate the sermorelin vial until the lyophilized powder is completely dissolved. 

Once the peptide is reconstituted, keep the vial refrigerated.

Sermorelin FAQ

How to Take Sermorelin?

Sermorelin is typically administered twice per day, in the morning prior to activity, and evening prior to bedtime. Doses are ideally administered on an empty stomach. As noted in the dosage section, it is common to administer between 200mcg to 600mcg per day.

How is Sermorelin Delivered?

Sermorelin is delivered via subcutaneous injection. 

Is Sermorelin Dangerous?

No, sermorelin has an excellent safety profile that has been demonstrated across several clinical trials that culminated in two FDA approvals. The most common side effects related to sermorelin are due to injection site pain and irritation. 

Is Sermorelin a Steroid?

No, sermorelin is a peptide that mimics the biological activity of GHRH. Although sermorelin produces similar physiological effects to anabolic steroids around muscle gain and fat loss, it operates via a separate pathway. 

Does Sermorelin Increase Testosterone?

Sermorelin has not been shown to directly increase testosterone. However, a 2017 study in which sermorelin was administered alongside GHRP-2 and GHRP-6 did show a statistically significant increase in testosterone levels. Sermorelin’s specific role in increasing testosterone has not been established.

Does Sermorelin Build Muscle?

Sermorelin has been shown to drive increased lean body mass and is hypothesized to do so via upregulation of GH and IGF-1. IGF-1 in particular has been shown to drive muscle gain through increased protein synthesis and amino acid uptake. 

Does Sermorelin Cause Weight Gain?

Sermorelin has not been shown to cause weight gain and has instead been shown to cause fat loss, particularly in the midsection. 

Sermorelin | Summary

Sermorelin mimics the biological activity of GHRH, which is responsible for inducing GH and subsequent IGF-1 secretion. As a result, sermorelin provides another approach to reaping the various benefits promised by recombinant human growth hormone therapy (rhGH) that are out of reach for most populations due to safety considerations. 

Because sermorelin leverages the natural GH secretion pathway, all GH and subsequent IGF-1 production induced by sermorelin is regulated and maintained within physiological ranges. 

This critical differentiating factor for sermorelin may allow users to experience therapeutic GH replacement without the prohibitive side effects associated with rhGH therapy. 

To source research-grade sermorelin, qualified researchers can trust Peptide Sciences.

References

1.    Corpas, E., Harman, S. M., Piñeyro, M. A., Roberson, R., & Blackman, M. R. (1992). Growth hormone (GH)-releasing hormone-(1-29) twice daily reverses the decreased GH and insulin-like growth factor-I levels in old men. The Journal of clinical endocrinology and metabolism, 75(2), 530–535. https://doi.org/10.1210/jcem.75.2.1379256

2.    Ishida, J., Saitoh, M., Ebner, N., Springer, J., Anker, S., von Haehling. (2020). Growth hormone secretagogues: history, mechanism of action, and clinical development. JSCM Rapid Communications. 3(1), 25-37. https://doi.org/10.1002/rco2.9 

3.    Thorner, M., Rochiccioli, P., Colle, M., Lanes, R., Grunt, J., Galazka, A., Landy, H., Eengrand, P., & Shah, S. (1996). Once daily subcutaneous growth hormone-releasing hormone therapy accelerates growth in growth hormone-deficient children during the first year of therapy. Geref International Study Group. The Journal of clinical endocrinology and metabolism, 81(3), 1189–1196. https://doi.org/10.1210/jcem.81.3.8772599 

4.    Walker R. F. (2006). Sermorelin: a better approach to management of adult-onset growth hormone insufficiency?. Clinical interventions in aging, 1(4), 307–308. https://doi.org/10.2147/ciia.2006.1.4.307 

5.    Prakash, A., & Goa, K. L. (1999). Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy, 12(2), 139–157. https://doi.org/10.2165/00063030-199912020-00007

6.    Barron, J. L., Coy, D. H., & Millar, R. P. (1985). Growth hormone responses to growth hormone-releasing hormone (1-29)-NH2 and a D-Ala2 analog in normal men. Peptides, 6(3), 575–577. https://doi.org/10.1016/0196-9781(85)90124-x

7.    Carroll, P. V., Christ, E. R., Bengtsson, B. A., Carlsson, L., Christiansen, J. S., Clemmons, D., Hintz, R., Ho, K., Laron, Z., Sizonenko, P., Sönksen, P. H., Tanaka, T., & Thorne, M. (1998). Growth hormone deficiency in adulthood and the effects of growth hormone replacement: a review. Growth Hormone Research Society Scientific Committee. The Journal of clinical endocrinology and metabolism, 83(2), 382–395. https://doi.org/10.1210/jcem.83.2.4594 

8.    Bowers, C. Y., Laferrére, B., Hurley, L., & Veldhuis, J. D. (2008). The role of growth hormone secretagogues and ghrelin in feeding and body composition In P. A. Donohoue  (Eds.), Contemporary Endocrinology: Energy Metabolism and Obesity: Research and Clinical Applications (pp. 125–154). Totowa, NJ: Humana Press.

9.    Sigalos, J. T., Pastuszak, A. W., Allison, A., Ohlander, S. J., Herati, A., Lindgren, M. C., & Lipshultz, L. I. (2017). Growth Hormone Secretagogue Treatment in Hypogonadal Men Raises Serum Insulin-Like Growth Factor-1 Levels. American journal of men's health, 11(6), 1752–1757. https://doi.org/10.1177/1557988317718662

10.    Merriam, G. R., Schwartz, R. S., & Vitiello, M. V. (2003). Growth hormone-releasing hormone and growth hormone secretagogues in normal aging. Endocrine, 22(1), 41–48. https://doi.org/10.1385/ENDO:22:1:41

11.    Valetto, M. R., Bellone, J., Baffoni, C., Savio, P., Aimaretti, G., Gianotti, L., Arvat, E., Camanni, F., & Ghigo, E. (1996). Reproducibility of the growth hormone response to stimulation with growth hormone-releasing hormone plus arginine during lifespan. European journal of endocrinology, 135(5), 568–572. https://doi.org/10.1530/eje.0.1350568

12.    Corpas, E., Harman, S. M., Piñeyro, M. A., Roberson, R., & Blackman, M. R. (1993). Continuous subcutaneous infusions of growth hormone (GH) releasing hormone 1-44 for 14 days increase GH and insulin-like growth factor-I levels in old men. The Journal of clinical endocrinology and metabolism, 76(1), 134–138. https://doi.org/10.1210/jcem.76.1.8421077

13.    Vitiello, M. V., Moe, K. E., Merriam, G. R., Mazzoni, G., Buchner, D. H., & Schwartz, R. S. (2006). Growth hormone releasing hormone improves the cognition of healthy older adults. Neurobiology of aging, 27(2), 318–323. https://doi.org/10.1016/j.neurobiolaging.2005.01.010

14.    Baker, L. D., Barsness, S. M., Borson, S., Merriam, G. R., Friedman, S. D., Craft, S., & Vitiello, M. V. (2012). Effects of growth hormone–releasing hormone on cognitive function in adults with mild cognitive impairment and healthy older adults: results of a controlled trial. Archives of neurology, 69(11), 1420–1429. https://doi.org/10.1001/archneurol.2012.1970

15.    The prohibited list [Internet]. World Anti Doping Agency. 2023 [cited 2023Feb8]. Available from: https://www.wada-ama.org/en/prohibited-list 

16.    The UFC Prohibited List [Internet]. USADA. 2023 [cited 2023Feb8]. Available from: https://ufc.usada.org/wp-content/uploads/2023-UFC-Prohibited-List.pdf 

17.    Gianturco, S., Pavlech, L., Storm, K. (2020). Sermorelin acetate: Summary Report. University of Maryland Center of Excellence in Regulatory Science and Innovation. 1-15. https://archive.hshsl.umaryland.edu/handle/10713/14877 

Disclaimer: The above is a sponsored post, the views expressed are those of the sponsor/author and do not represent the stand and views of Outlook Editorial.

 

Important: We are happy to announce that we have successfully completed the migration of our site @outlookindia.com to enhance your experience as valuable user. But due to the scale of operations some data discrepancies may arise. We apologize for any inconvenience and thank you for your patience and understanding during this period.
Advertisement
Advertisement
Advertisement
Advertisement
Advertisement