Sermorelin Acetate ODT

Sermorelin is a synthetic peptide that serves as an analog of Growth Hormone-Releasing Hormone (GHRH), a naturally occurring neurohormone produced in the hypothalamus.^[1][2][3][4]

Sermorelin is comprised of the first 29 amino acids of GHRH, making it a potential agent for stimulating growth hormone (GH) secretion from the anterior pituitary gland.^[2][3]

This mechanism has implications for assisting with growth hormone deficiencies (GHD) in both children and adults.^[2]

Growth Hormone Deficiency (GHD)

Sermorelin may assist in stimulating endogenous GH production in children with GHD and adults with GH insufficiency.^[2]

Emerging Potential in Hypogonadism

A study in short children suggested sermorelin may help increase not only GH, but also prolactin, FSH, and LH. The study observed small acute changes in these hormones after sermorelin administration.^[2]

In rats, a study suggested sermorelin administration may lead to an increase in testosterone production. However, trials in humans have not shown significant changes in testosterone levels.^[2]

Anti-Aging and Metabolic Health

Natural GH levels decline with age. Low levels of growth hormone may contribute to age-related changes such as reduced lean body mass, increased adiposity, diminished bone density, and thin dry skin.^[5]

Sleep Regulation

An animal study suggested acute replacement of GHRH may positively influence sleep patterns by potentially increasing slow-wave sleep (SWS), or “deep sleep”.^[6]

Receptor Binding and Signaling Pathways

Sermorelin may bind to GHRH receptors (GHRHR) and impact the hypothalamic-pituitary-somatotropic axis to promote GH secretion.^[2]

This interaction activates intracellular pathways, specifically the Gs protein/adenylate cyclase and mitogen-activated protein kinase pathways, which leads to the formation of cAMP.^[2]

Unlike exogenous GH administration, sermorelin may help preserve the pituitary’s intermittent secretion pattern, mimicking physiological GH rhythms observed with endogenous GHRH.^[2][7]

Physiological Effects of GH Release

GH release stimulates insulin-like growth factor 1 (IGF-1) production, a critical regulator of GH through negative feedback inhibition.^[3]

Physiologically, animal studies have suggested IGF-1 plays a role in growth after birth. Interestingly, in human adults, both high and low levels of serum IGF-1 are associated with high mortality.^[3]

A clinical study in elderly men suggested that sermorelin therapy may increase IGF-1 levels in a dose-dependent manner.^[2]

The study examined twice-daily sermorelin administration in elderly men. The study suggested sermorelin restored IGF-1 concentrations to levels closer to those of younger men, with elevated levels persisting for up to two weeks post-administration.^[2]

Contraindications

Hypersensitivity Reactions

Sermorelin is contraindicated in patients with a known hypersensitivity to sermorelin acetate or any excipients in the formulation. Allergic reactions may manifest as hives, rash, or anaphylaxis requiring immediate discontinuation and medical intervention.^[11]

Active Malignancies

Tesamorelin, a medication that also stimulates GHRH receptors, is contraindicated in patients with active or recurrent malignancies due to its potential to elevate insulin-like growth factor 1 (IGF-1), which may stimulate tumor growth. [8] Sermorelin may increase IGF-1, which may pose a risk in this patient population.^[2][8]

Pregnancy and Lactation

Sermorelin is classified under *Pregnancy Category C*, as animal studies have shown fetal variations at high doses.^[9]

Human data is insufficient, and the risks to fetal development remain uncertain. Sermorelin should also be avoided in breastfeeding patients, as its excretion in human milk is unknown.^[1][9][10]

Hypothalamic-Pituitary Axis Disruption

Patients with structural hypothalamic or pituitary abnormalities (e.g., tumors, post-surgical damage, or hypophysectomy) are not candidates for medications classified as growth hormone-releasing agonists. These drugs require an intact pituitary gland to stimulate growth hormone (GH) secretion.^{[8] [11]}

Untreated Hypothyroidism

Untreated hypothyroidism may impair sermorelin’s potential.^[1][8]

Precautions

Thyroid Function

Regular monitoring of thyroid function is needed, as untreated hypothyroidism may compromise potential response.^[1][9]

Drug Interactions

Sermorelin may interact with other medications including glucocorticoids (e.g., prednisone), cyclooxygenase inhibitors (e.g., aspirin), and thyroid hormones (e.g., levothyroxine).^[10][11]

IGF-1 and Glucose Monitoring

Sermorelin may help increase IGF-1 levels, which may require periodic serum testing as both low and high IGF-1 levels have been linked to cardiovascular risks in certain patient populations.^[12]

GH secretion may exacerbate insulin resistance, so patients may require frequent glucose monitoring, especially those with diabetes or prediabetes.^[3]

Injection Site Reactions

Subcutaneous administration may cause localized pain or irritation. Proper injection technique—rotating sites and using sterile practices—minimizes discomfort and helps prevent complications.^[13]

Critical Illness Considerations

Sermorelin is not recommended for patients with acute critical illnesses (e.g., postoperative complications or respiratory failure), as GH modulation may increase mortality risk in these populations.^[14]

Special Populations

Sermorelin’s use in patients with growth hormone deficiency due to intracranial lesions is unestablished. Sermorelin should be avoided in this patient population.^[9]

Geriatric Use

Older adults may be more susceptible to certain potential side effects of growth hormone replacement, including fluid retention and arthralgia. Dosage adjustments may be necessary to mitigate these potential side effects.^[5]

Common Adverse Reactions

Injection Site Reactions

Injection site reactions are possible at the administration site, including swelling, redness, irritation or pain.^[1][13]

Rotating injection sites and ensuring proper technique may mitigate these reactions.^[1][13]

Less Frequent Systemic Reactions

Neurological and Gastrointestinal Symptoms

Headaches, dizziness, restlessness, and sleepiness are occasionally reported.^[1] Mild gastrointestinal disturbances, such as nausea, may occur.^[8]

Immunogenicity

Anti-GRF antibodies may develop in a subset of patients while using sermorelin, though clinical significance remains unclear. Antibody presence does not appear to correlate with potential response to sermorelin or hypersensitivity in most cases.^[9]

Serious Adverse Events

Hypersensitivity Reactions

Rare cases of urticaria, angioedema, or anaphylaxis have been documented. Immediate discontinuation and seeking immediate medical attention are advised if signs of systemic allergy (e.g., difficulty breathing, chest tightness, facial swelling) emerge.^[9][10][15]

Special Populations

Pregnancy and Lactation

Sermorelin is classified as **Pregnancy Category C**. Animal studies show fetal variations. There is no adequate data on use in pregnant women. It is not known if sermorelin passes into breast milk. Due to this potential risk, use should be avoided in breast-feeding women.^[9]

Drug Interactions

Potential interactions may include glucocorticoids (e.g., prednisone) or cyclooxygenase inhibitors (e.g., aspirin).^[10]

Below is a list of other potential drug interactions:

Amphetamine/dextroamphetamine

Alcohol (ethanol)

Aspirin

Lorazepam

Tadalafil

Clomiphene

CoQ10 (ubiquinone)

Rosuvastatin

Duloxetine

Testosterone

DHEA (dehydroepiandrosterone)

Apixaban

Fish Oil (omega-3 polyunsaturated fatty acids)

Fish Oil Ultra (omega-3 polyunsaturated fatty acids)

Flomax (tamsulosin)

HCG (chorionic gonadotropin)

L-Arginine (arginine)

L-Carnitine (levocarnitine)

Escitalopram

Eszopiclone

Quetiapine

Levothyroxine

Acetaminophen

Valacyclovir

Cyanocobalamin

Ascorbic acid

Cholecalciferol

Lisdexamfetamine

Bupropion

Cetirizine

Insulin

^[15]

Pregnancy

Sermorelin is classified under *Pregnancy Category C* based on animal studies.^[9]

In rats and rabbits, sermorelin administration resulted in fetal variations.^[9]

No adequate human studies exist to confirm these findings or evaluate use pregnant women.^[9][11]

Patient Counseling

Healthcare providers should advise patients to disclose pregnancy status before initiating treatment. Withholding this information may lead to adverse outcomes.

Breastfeeding

It is unknown if sermorelin passes into human breast milk.^[9][10]

Breastfeeding should be avoided during sermorelin use due to unknown excretion risks.^[9][10]

Alternatives: Non-pharmacologic interventions or alternative therapies may be considered for lactating patients requiring GH modulation.

Key Precautions

Patient Disclosure

Patients must inform providers if they are pregnant, planning pregnancy, or breastfeeding. Inaccurate health disclosures may increase risks of fetal harm or infant complications.

Diagnostic Testing

A pregnancy test is recommended for women of reproductive age before starting sermorelin.^[1]

Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond use date. Do not flush unused medications or pour down a sink or drain.

1. Olarescu NC, Gunawardane K, Hansen TK, et al. Normal Physiology of Growth Hormone in Adults. [Updated 2019 Oct 16]. In: Feingold KR, Anawalt B, Blackman MR, et al., editors. Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.; 2000-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK279056/
2. Garcia, J. M., Merriam, G. R., & Kargi, A. Y. (2019, October 7). Growth hormone in aging. Endotext – NCBI Bookshelf. https://www.ncbi.nlm.nih.gov/books/NBK279163/
3. Vitiello, M. V., Schwartz, R. S., Moe, K. E., Mazzoni, G., & Merriam, G. R. (2001). Treating age-related changes in somatotrophic hormones, sleep, and cognition. Dialogues in Clinical Neuroscience, 3(3), 229–236. https://doi.org/10.31887/dcns.2001.3.3/mvvitiello
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 PMID: 18046908; PMCID: PMC2699646
5. Sinha, D. K., Balasubramanian, A., Tatem, A. J., Rivera-Mirabal, J., Yu, J., Kovac, J., Pastuszak, A. W., & Lipshultz, L. I. (2020). Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males. Translational Andrology and Urology, 9(S2), S149–S159. https://doi.org/10.21037/tau.2019.11.30
6. Healthline. (2022, April 27). *Sermorelin therapy benefits, uses, side effects, risks, more*. https://www.healthline.com/health/sermorelin
7. Chang, Y., Huang, R., Zhai, Y., Huang, L., Feng, Y., Wang, D., Chai, R., Zhang, W., & Hu, H. (2021). A potentially effective drug for patients with recurrent glioma: sermorelin. Annals of Translational Medicine, 9(5), 406. https://doi.org/10.21037/atm-20-6561
8. RxList. (2022, October 24). *Sermorelin acetate*. https://www.rxlist.com/sermorelin-acetate-drug.htm
9. U.S. Food and Drug Administration. (2019). *EGRIFTA SV prescribing information*. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022505s012s013lbl.pdf
10. Mayo Clinic. (2025, February 1). *Sermorelin (injection route)*. https://www.mayoclinic.org/drugs-supplements/sermorelin-injection-route/description/drg-20065923
11. Drugs.com. (n.d.). *Sermorelin interactions*. https://www.drugs.com/drug-interactions/sermorelin.html
12. Carlzon D, Svensson J, Petzold M, Karlsson MK, Ljunggren Ö, Tivesten Å, Mellström D, Ohlsson C. Both low and high serum IGF-1 levels associate with increased risk of cardiovascular events in elderly men. J Clin Endocrinol Metab. 2014 Nov;99(11):E2308-16. doi: 10.1210/jc.2014-1575. Epub 2014 Jul 24. PMID: 25057875; PMCID: PMC4258605.
13. Takala, J., Ruokonen, E., Webster, N. R., Nielsen, M. S., Zandstra, D. F., Vundelinckx, G., & Hinds, C. J. (1999). Increased Mortality Associated with Growth Hormone Treatment in Critically Ill Adults. New England Journal of Medicine, 341(11), 785–792. https://doi.org/10.1056/nejm199909093411102
14. Kim J, De Jesus O. Medication Routes of Administration. [Updated 2023 Aug 23]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2025 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK568677/
15. Drugs.com. (2025). *Sermorelin acetate: Indications, side effects, warnings*. https://www.drugs.com/cdi/sermorelin-acetate.html