Sermorelin — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for Sermorelin, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GHRH receptor (GHRHR) | Agonist | Full agonist activity equivalent to native GHRH(1-44) |
§2.2Mechanism of action
Sermorelin stimulates pituitary growth-hormone release through the GHRH receptor. Its very short half-life confines the pharmacodynamic effect to a single secretory pulse, which is why its established clinical use was diagnostic — as a provocative test of pituitary somatotroph reserve — rather than therapeutic.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈11–12 min
- Time to maximum concentration
- ≈5–20 min (intravenous), 15–30 min (subcutaneous)
- Volume of distribution
- ≈24–32 L
- Plasma protein binding
- not extensively bound
- Clearance
- high
- Bioavailability
- not formally established
Rapid cleavage at the Tyr1-Ala2 bond by dipeptidyl peptidase-4, producing the inactive GRF(3-29) fragment, followed by further proteolysis.
§2.4Interactions
- Glucocorticoids, thyroid hormone, somatostatin analogues, muscarinic antagonists and cyclo-oxygenase inhibitors all modify the growth-hormone response and confound diagnostic use
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Prakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs 1999;12(2):139–157. doi:10.2165/00063030-199912020-00007 · PMID 18031173
- Falutz J, Allas S, Blot K, Potvin D, Kotler D, Somero M, Berger D, Brown S, Richmond G, Fessel J, Turner R, Grinspoon S. Metabolic effects of a growth hormone-releasing factor in patients with HIV. New England Journal of Medicine 2007;357(23):2359–2370. doi:10.1056/NEJMoa072375 · PMID 18052660
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.