Sermorelin

Research · Sermorelin

Overview

Sermorelin (GRF 1-29 NH2) is a synthetic 29-residue analog corresponding to the N-terminal fragment of endogenous growth hormone-releasing hormone, the shortest sequence retaining full biological activity. It was developed in the 1980s and was approved for clinical use in several jurisdictions, and was used in diagnostic research on pituitary growth hormone reserve before commercial discontinuation in the United States. It is used as a reference GHRH receptor agonist in somatotropic axis research.

Mechanism of action

Binds and activates the GHRH receptor, a class B G-protein-coupled receptor expressed on anterior pituitary somatotrophs. Activation of Gs-coupled adenylyl cyclase raises intracellular cAMP and activates protein kinase A, which phosphorylates CREB and increases transcription of the growth hormone gene and the Pit-1 transcription factor. Calcium influx then triggers release of stored hormone. Because sermorelin acts upstream of the pituitary, the resulting growth hormone release remains pulsatile and subject to negative feedback from somatostatin and circulating IGF-1. The unmodified native sequence is rapidly cleaved by DPP-4, giving a plasma half-life of minutes.

Key research findings

1. 01

   Clinical studies in children with idiopathic growth hormone deficiency characterized increases in growth velocity, reviewed in the context of diagnostic research and long-term studies.

2. 02

   Diagnostic research established its use as a provocative test of pituitary somatotroph reserve, distinguishing hypothalamic from pituitary causes of deficiency.

3. 03

   Studies in older adults characterized restoration of nocturnal growth hormone pulsatility and increases in IGF-1 concentrations, reviewed as an approach to adult-onset growth hormone insufficiency.

4. 04

   Pharmacokinetic studies document rapid N-terminal cleavage and a short plasma half-life, motivating the development of stabilized analogs such as modified GRF (1-29) and tesamorelin.

Published references

• Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency

  Prakash A et al. — BioDrugs, 1999 · PMID: 18031173

• Sermorelin: a better approach to management of adult-onset growth hormone insufficiency?

  Walker RF — Clin Interv Aging, 2006 · PMID: 18046908

The information above is derived from published preclinical and clinical research. It is provided for educational purposes only and does not constitute medical advice, diagnosis, or treatment recommendations.