Sermorelin acetate is a synthetic analog of naturally occurring Growth Hormone-Releasing Hormone (GHRH). GHRH is produced in an area of the brain called the hypothalamus from which it is released into blood vessels that carry it to the pituitary gland. Once there, it stimulates production and secretion of growth hormone (GH) which is necessary for growth and development during childhood, as well as for maintenance of normal body composition and metabolism in adults. When GH concentrations are low, deficiency causes poor growth, inadequate muscle and bone development, as well as increased risk for development of intrinsic diseases such as diabetes and other pathologies. Such deficiencies can be opposed by administration of sermorelin which stimulates the pituitary gland to increase output of GH and thereby elevate and restore its serum concentrations to normal levels.
After Roger Guillemin and Andrew Schally were awarded the 1977 Nobel Prize in Medicine for their work on neuroendocrine releasing factors, the precise chemical structure of GHRH, a 44 amino acid peptide, was determined using tissue from human pancreatic tumors that caused acromegaly, a disease resulting from excess secretion of GH.1 The following year, Wehrenberg and Ling2 sought to determine which part of the molecule was essential for its pituitary stimulating action. By eliminating individual amino acids and then testing the remaining peptide fragments, they found that only the first 29 amino acids are needed for stimulating pituitary production and secretion of HGH. Consequently, this fragment of the native molecule, commonly known as Sermorelin is often used to treat GH deficient states in children and adults
Chemically, sermorelin is known as growth hormone releasing factor (GRF) or growth hormone releasing hormone (GRH)1-29 NH2 indicating that the amino terminus is at position 29. However, the molecule is not used clinically as the free base, but rather as the acetic acid salt, i.e. as sermorelin acetate. The free base of sermorelin has the empirical formula C149H246N44O42S and a molecular weight of 3,358 daltons3 Sermorelin acetate is a sterile, non-pyrogenic, lyophilized powder intended for subcutaneous injection after reconstitution with Bacteriostatic Water for Injection and should be stored at between 36 and 46° F (2 and 8° C). Taxonomically, sermorelin is listed as an organic compound (kingdom), an organic acid (superclass), a carboxylic acid (class), amino acid/peptide analogue (subclass), and as a peptide (direct parent).4
Sermorelin is available from Empower Pharmacy in general (non-customized) vials containing 3.0 mg, 6.0 mg, 9.0 mg and 15.0 mg each. Because of its ability to bind receptors on somatotrophs, the pituitary cells that produce and secrete GH, sermorelin has several clinical indications and applications related to GHRH/GH insufficiency.5 For example it is officially indicated and approved for diagnostic evaluation of pituitary function and also for treatment of delayed or inadequate growth in children. It also can be used to oppose maladaptive changes in body composition such as reduced lean body mass (muscle), increased total and visceral fat, and decreased bone mass resulting from low or inadequate concentrations of serum GH and insulin-like growth factor-1 (IGF-1).
Data from research and clinical studies have demonstrated sermorelin’s multifaceted properties, some of which include:
- Peak increases in hGH followed administration of GHRH analogs after 15 or 30 min. An increase in the integrated plasma growth hormone (GH) response was observed at each dose.6
- Quality of life parameters including general well-being (P < 0.05) and libido (P < 0.01) significantly improved in men receiving sermorelin therapy.7
- Youthful concentrations and patterns of serum hGH were restored in older persons by daily injections of GRF (sermorelin).8
- Body composition improved after regular administration of GRF for 90 days resulting in increased muscle mass, increased total body water and decreased visceral fat.9
- Quality of sleep improved as indicated by extended Stage IV and Slow Wave Sleep in men.10
- 1. Rivier J, Spiess J, Thorner M, Vale W. 1982 Characterization of a growth hormone-releasing factor from a human pancreatic islet tumour. Nature, 300:276-278.
- 2. Wehrenberg WB, Ling N (1983). "In vivo biological potency of rat and human growth hormone-releasing factor and fragments of human growth hormone-releasing factor". Biochem Biophys Res Commun. 115 (2): 525–530.
- 3. Drug Bank, Sermorelin, Identification. Drug created on June 13, 2005 07:24 / Updated on January 20, 2014 14:07 http://www.drugbank.ca/drugs/DB00010
- 4. Drug Bank, Sermorelin, Identification. Drug created on June 13, 2005 07:24 / Updated on January 20, 2014 14:07 http://www.drugbank.ca/drugs/DB00010
- 5. Drug Bank, Sermorelin, Pharmacology. Drug created on June 13, 2005 07:24 / Updated on January 20, 2014 14:07 http://www.drugbank.ca/drugs/DB00010
- 6. Barron JL, Coy DH, Millar RP Growth hormone responses to growth hormone-releasing hormone (1-29)-NH2 and a D-Ala2 analog in normal men. Peptides. 1985 May-Jun, 6(3):575-577.
- 7. 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-advancing men and women. J Clin Endocrinol Metab. 1997 May; 82(5):1472-9.
- 8. Corpas E, Harman SM, Pineyro MA et al. 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, 75:530-535.
- 9. Veldhuis JD, Patrie JM, Frick K, et al. Administration of recombinant GHRH for 3 months reduces abdominal visceral fat mass and icnreases physical performance measures in postmenopausal women. Eur J Endocrinol. 2005, 153:669-677.
- 10. Steiger A, Guldner J, Hemmeter U, Rothe B, Wiedemann K, Holsboer F. Effects of growth hormone-releasing hormone and somatostatin on sleep EEG and nocturnal hormone secretion in male controls. Neuroendocrinology. 1992 Oct; 56(4):566-73.