Sermorelin

Chemical & identity

Sequence

YADAIFTNSYRKVLGQLSARKLLQDIMSR

Length

29 residues

Molecular formula

C149H246N44O42S

Molecular weight

3357.9 g/mol · PubChem

PubChem CID

16132413 · PubChem

SMILES

CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CC=C(C=C3)O)N

InChIKey

WGWPRVFKDLAUQJ-MITYVQBRSA-N

ChEMBL ID

CHEMBL1201490 · ChEMBL

UniProt

P01286 · UniProt

Category

GH secretagogue/GHRH

Chemical/structural fields are auto-pulled and source-linked. ChEMBL data: ChEMBL_36, CC BY-SA 3.0.

Mechanism (curated)

Synthetic analog of growth-hormone-releasing hormone (GHRH residues 1-29); binds pituitary GHRH receptors to stimulate endogenous GH secretion.

Pharmacology & handling

Half-life

Approximately 10-15 minutes (very short); administered subcutaneously.

Research

• A potentially effective drug for patients with recurrent glioma: sermorelin.

  Human trial

  Chang Y et al. · Annals of translational medicine · 2021 · Cohort

  This cohort study of 1,018 glioma patients analyzed transcriptomics data to screen for drugs effective against recurrent gliomas. Using a Drug Resistant Scores approach applied to 4,865 drugs, the analysis identified sermorelin as the drug to which recurrent glioma patients were most sensitive. Pathway analysis suggested sermorelin may work by blocking cell cycle progression and modulating immune responses, including effects on immune checkpoints and M0 macrophages. The benefit appeared most relevant for recurrent patients with high-grade, IDH-wildtype, and 1p/19q non-codeletion status, and Kaplan-Meier analysis suggested benefit independent of adjuvant treatment.

  DOIPubMed 33842627Free full text (cc-by-nc-nd)

• PEGylation of growth hormone-releasing hormone (GRF) analogues.

  Animal-only

  Esposito P et al. · Advanced drug delivery reviews · 2003 · Other

  This study examines PEGylation of sermorelin (GRF1-29), a synthetic peptide identical to the first 29 amino acids of natural GHRH, to address its short plasma half-life of 10-20 minutes in humans caused by renal filtration and enzymatic degradation. Different PEGylated GRF conjugates were tested in vitro and in vivo using rat and pig models, with GH serum levels monitored after intravenous or subcutaneous injection. Mono-PEGylated variants with PEG5000 linked to Lys 12 or Lys 21 demonstrated bioactivity similar to native sermorelin in vitro but showed higher pharmacodynamic response compared to unmodified GRF. The study investigated how PEG molecular weight, number of PEG chains, and PEGylation position affected sermorelin activity.

  DOIPubMed 14499707

• Clinical review: Is lack of recombinant growth hormone (GH)-releasing hormone in the United States a setback or time to consider glucagon testing for adult GH deficiency?

  Human trial

  Yuen KC et al. · The Journal of clinical endocrinology and metabolism · 2009 · Narrative review

  This clinical review examines alternatives to the GHRH-ARG stimulation test for diagnosing adult GH deficiency after the 2008 discontinuation of recombinant GHRH (Geref) in the United States. The authors reviewed published data and consensus guidelines to assess the reliability and discriminatory value of various GH stimulation tests, including glucagon, arginine, and GH secretagogues. They conclude that the insulin tolerance test should remain the first-line diagnostic test, but recommend the glucagon stimulation test as the preferred alternative when ITT is not feasible and recombinant GHRH is unavailable. The review notes that further studies into simpler, comparable alternatives to ITT are needed.

  DOIPubMed 19509104Free full text

• Synthesis and structure-activity studies on novel analogs of human growth hormone releasing hormone (GHRH) with enhanced inhibitory activities on tumor growth.

  Animal-only

  Zarandi M et al. · Peptides · 2017 · Other

  This study describes the synthesis and evaluation of novel GHRH analogs of the Miami (MIA) series, designed with multiple amino acid substitutions to enhance anticancer activity. The analogs were tested for growth hormone release activity in rat pituitary cells and in vivo in rats, receptor binding affinity in vitro, and inhibitory effects on tumor proliferation in multiple human cancer cell lines (endometrial, colorectal, prostate) and in nude mice xenografted with various human cancers. Several analogs (MIA-602, MIA-604, MIA-610, MIA-640) demonstrated high binding affinity and strong inhibitory activity on tumor growth in vitro and in vivo, with MIA-602 showing potent suppression across multiple cancer types. The authors suggest that tumor growth suppression may be partly mediated by downregulation of GHRH receptor levels, and note that these analogs have only weak endocrine GH-inhibitory activity.

  DOIPubMed 28130121

• GH feedback occurs through modulation of hypothalamic somatostatin under cholinergic control: studies with pyridostigmine and GHRH.

  Human trial

  Ross RJ et al. · Clinical endocrinology · 1987 · Other

  A human study in six healthy male volunteers examined how increased cholinergic tone affects growth hormone (GH) response to GHRH (sermorelin). Pyridostigmine, an acetylcholinesterase inhibitor, increased basal GH secretion and augmented the GH response to intravenous GHRH (1-29) NH2, with a synergistic effect beyond the sum of each agent alone. When methionyl-hGH pretreatment suppressed the GH response to GHRH, pyridostigmine restored this response, suggesting that GH negative feedback operates through hypothalamic somatostatin secretion under inhibitory cholinergic control.

  DOIPubMed 2901302

Summaries are our own; we link to originals (PubMed / DOI) and never rehost full text.

Regulatory status

FDA approved

No

WADA prohibited

Yes

Compounding status

Previously FDA-approved (Geref); withdrawn from the US market for commercial reasons (not safety). Available via compounding.

Notes

Formerly FDA-approved as Geref for GH-deficiency diagnosis/treatment; withdrawn from the US market for commercial (non-safety) reasons. Prohibited in sport under WADA (GHRH analog), as of 2026-06-04.

Legal/regulatory status varies by jurisdiction and changes over time — accurate as of last review (2026-06-04).