Sermorelin
approvedAlso known as: GHRH (1-29), GRF 1-29
**Mechanism of Action** Sermorelin (GHRH 1-29) is a synthetic analog of endogenous growth hormone-releasing hormone (GHRH), comprising the first 29 amino acids of the native 44-amino acid peptide. It binds specifically to GHRH receptors on anterior pituitary somatotroph cells, activating the cAMP/PKA signaling pathway to stimulate pulsatile secretion of growth hormone (GH). This pulsatile release mimics physiological GH patterns, distinguishing it from continuous GH administration. Sermorelin does not directly elevate GH levels but enhances the amplitude and frequency of endogenous GH pulses, thereby preserving negative feedback regulation via somatostatin and IGF-1. **Key Research Findings** Approved by the FDA for diagnostic use in GH deficiency (GHD) and as a therapeutic agent in children with idiopathic GHD, clinical studies demonstrate that sermorelin increases GH and IGF-1 levels in a dose-dependent manner. In adults with relative GHD, trials show improvements in lean body mass, bone density, and lipid profiles, though effects on muscle strength and cognitive function remain inconsistent. Long-term safety data indicate low immunogenicity and minimal adverse effects (e.g., transient injection-site reactions, mild hyperglycemia). However, efficacy in age-related GH decline is limited, as pituitary responsiveness diminishes with aging. **Clinical Relevance** Sermorelin is primarily used off-label for GH stimulation testing and as an alternative to recombinant GH in pediatric GHD, offering a more physiological approach with reduced risk of supraphysiological IGF-1 levels. Its utility in anti-aging or sports performance contexts lacks robust evidence and is not FDA-approved. Contraindications include active malignancy, intracranial hypertension, and hypersensitivity. Monitoring of IGF-1 and glucose metabolism is recommended during therapy. For research purposes only — not medical advice.
Key data
C149H246N44O42SResearch & studies
GHRP-4, GHRP-6, and Sermorelin (22-29) were stable to enzyme and blood treatment.; These three peptides can serve as in-house internal standards for peptide quantification.; GHRP-6 and Sermorelin (22-29) were used to analyze a dimeric peptide in four different matrices.; A unique protein binding and enzymatic stability profile was established for each peptide.
First separation of GHRH enantiopeptides (sermorelin and CJC-1293) differing by one chiral amino acid.; PS-LVSS with 80% capillary volume injection outperformed sweeping in signal enhancement.; Adding 0.1 mM phosphoric acid with 30% methanol to sample doubled signal compared to water.; Method achieved 640-fold signal enhancement in desalted urine versus CZE without preconcentration.
Recurrent glioma patients showed highest sensitivity to sermorelin in high-throughput drug screening.; Sermorelin was effective for recurrent patients with high grade, IDH-wildtype, and 1p/19q non-codeletion status.; Sermorelin may inhibit tumor cell proliferation through cell cycle blocking and negatively regulate immune checkpoints and M0 macrophages.; Patient benefit from sermorelin was independent of postoperative adjuvant treatment.
PEGylation of GRF1-29 extends its in vivo half-life by reducing renal ultrafiltration and enzymatic degradation.; Mono-PEGylated isomers with PEG5000 at Lys12 or Lys21 exhibited in vitro bioactivity similar to unmodified hGRF1-29.; These PEGylated conjugates showed higher pharmacodynamic response (endogenous GH levels) compared to unmodified GRF in animal models.
Intravenous sermorelin 1 µg/kg is a rapid, relatively specific diagnostic test for growth hormone deficiency with fewer false positives than other tests.; Once daily subcutaneous sermorelin 30 µg/kg at bedtime effectively increases height velocity in prepubertal children with idiopathic growth hormone deficiency.; Sermorelin-induced catch-up growth was observed in most children, with good response in slow-growing, shorter children with delayed bone age.; Sermorelin is well tolerated, with transient facial flushing and injection site pain as common adverse events.
Frequently asked questions
What is Sermorelin?
**Mechanism of Action** Sermorelin (GHRH 1-29) is a synthetic analog of endogenous growth hormone-releasing hormone (GHRH), comprising the first 29 amino acids of the native 44-amino acid peptide. It binds specifically to GHRH receptors on anterior pituitary somatotroph cells, activating the cAMP/PKA signaling pathway
How does Sermorelin work?
GHRH(1-29) analog that binds pituitary GHRH receptors to stimulate pulsatile growth hormone release.
What is the research status of Sermorelin?
Sermorelin is currently classified as approved, with 25 research references on record. This is for research purposes only and is not medical advice.
What is the half-life of Sermorelin?
The reported half-life of Sermorelin is 10-20 minutes.
What is the molecular weight of Sermorelin?
Sermorelin has a molecular weight of approximately 3357.9 g/mol (formula C149H246N44O42S).
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