Sermorelin Acetate Injection

Overview of Sermorelin Acetate Injection

Dosage Strength

  • 6 mg Lyophilized Vial
  • 9 mg Lyophilized Vial
  • 15 mg Lyophilized Vial

General Information

Sermorelin is a structurally shortened version of Growth Hormone Releasing Hormone (GHRH). It is made up of the first 29 amino acids of a naturally occurring neurohormone made in the hypothalamus. 1 Sermorelin is the most commonly used GHRH analogue medication. It can considerably increase the synthesis and release of growth hormone (GH) from pituitary gland cells, improving serum levels of GH and, as a result, insulin-like growth factor 1 (IGF-1) in both animals and humans. 23 It has the ability to regulate a confluence of hormonal signals that affect GH secretion from the anterior pituitary, including GHRH, somatostatin, insulin-like growth factor (IGF), and others. A rhythmic-circadian pattern of GH secretion is created by the positive and negative opposing regulation of growth hormone by GHRH and somatostatin, respectively. 4 Sermorelin treatment thus modifies both the pulse amplitude and frequency of GH secretion. 5 Sermorelin promotes IGF-1 production in the liver and peripheral organs after stimulating GH release from the pituitary gland. 5

Sermorelin regulates cellular activity by acting on the pituitary growth hormone releasing hormone receptor (GHRHr). GHRHr is the endogenous hormone GHRH’s and sermorelin’s natural receptor. This receptor controls growth hormone release both directly and indirectly via feedback connections with somatostatin. 6

Sermorelin is rapidly degraded after entering the bloodstream, with a biological half-life of 10-20 minutes.7 Because of the biological half-life and bioavailability of Sermorelin, treatment for growth in children with GHD must be done on a regular basis, multiple times per day as subcutaneous injections. 8 However, most cases of adult-onset GH deficiency can be treated with a single daily dose. Three (3) mcg/kg subcutaneous Sermorelin injections have been observed to mimic naturally occurring GHRH-mediated GH release reactions. 9

GHRH impacts sleep patterns by increasing the quantity of slow wave sleep (SWS), boosting sleep-related GH secretion, and decreasing cortisol secretion in addition to increasing production and secretion. 10

Sermorelin requires a healthy pituitary gland and a variety of peripheral organs to work properly. 11 12 This is because endogenous receptors control hormone secreting glands and tissues. More specifically, functioning growth hormone releasing hormone receptors (GHRHr) on somatotrophs are necessary in a functioning anterior pituitary. 11

References

1.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.
2.Chen, R.G., et al., 1993. A comparative study of growth hormone (GH) and GH-releasing hormone (1-29)-NH2 for stimulation of growth in children with GH deficiency. Acta Paediatr Suppl, 388: p. 32-5; discussion 36.
3.Perez-Romero, A., et al., 1999. Effect of long-term GHRH and somatostatin administration on GH release and body weight in prepubertal female rats. J Physiol Biochem, 55(4): p. 315-24.
4.Tannenbaum, G.S. and Ling N. 1984. The interrelationship of growth hormone (GH)-releasing factor and somatostatin in generation of the ultradian rhythm of GH secretion. Endocrinology, 115(5): p. 1952-7.
5.Tauber, M.T., et al., 1993. Growth hormone (GH) profiles in response to continuous subcutaneous infusion of GH-releasing hormone(1-29)-NH2 in children with GH deficiency. Acta Paediatr Suppl, 388: p. 28-30; discussion 31.
6.Howard AD, Feighner SD, Cully DF et al. 1996, A Receptor in Pituitary and Hypothalamus That Functions in GH release. Science. Vol. 273, Issue 5277, pp. 974-977
7.Esposito, P., et al., 2003. PEGylation of growth hormone-releasing hormone (GRF) analogues. Adv Drug Deliv Rev, 55(10): p. 1279-91.
8.Kirk JM, Trainer PJ, Majrowski WH, Murphy J, Savage MO, Besser GM. 1994. Treatment with GHRH(1-29)NH2 in children with idiopathic short stature induces a sustained increase in growth velocity. Clin Endocrinol (Oxf). 41(4):487-93.
9.Aitman, T.J., et al., 1989. Bioactivity of growth hormone releasing hormone (1-29) analogues after SC injection in man. Peptides, 10(1): p. 1-4.
10.Steiger, A., et al., 1994. Growth hormone-releasing hormone (GHRH)-induced effects on sleep EEG and nocturnal secretion of growth hormone, cortisol and ACTH in patients with major depression. J Psychiatr Res, 28(3): p. 225-38.
11.Mayo, K.E., et al., 1995. Growth hormone-releasing hormone: synthesis and signaling. Recent Prog Horm Res, 50: p. 35-73.
12.Ceda, G.P., et al. 1987. The growth hormone (GH)-releasing hormone (GHRH)-GH-somatomedin axis: evidence for rapid inhibition of GHRH-elicited GH release by insulin-like growth factors I and II. Endocrinology, 120(4): p. 1658-62.
13.Mayo, K.E., et al., Growth hormone-releasing hormone: synthesis and signaling. Recent Prog Horm Res, 1995. 50: p. 35-73.
14.Ceda, G.P., et al., The growth hormone (GH)-releasing hormone (GHRH)-GH-somatomedin axis: evidence for rapid inhibition of GHRH-elicited GH release by insulin-like growth factors I and II. Endocrinology, 1987. 120(4): p. 1658-62.
15.Tannenbaum, G.S. and N. Ling, The interrelationship of growth hormone (GH)-releasing factor and somatostatin in generation of the ultradian rhythm of GH secretion. Endocrinology, 1984. 115(5): p. 1952-7.

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