Category
GH Secretagogues
GHRH analogs and ghrelin mimetics that stimulate growth hormone release.
CJC-1295 (no DAC)
Mod GRF 1-29 (CJC-1295 without DAC)
Short-acting GHRH analog (modified GRF 1-29) with ~30-min half-life. No published human PK trial. WADA-prohibited (S2), FDA Category 2 since September 2023.
CJC-1295 with DAC
CJC-1295 with Drug Affinity Complex (DAC)
Modified GHRH analog with maleimide DAC linker producing 6-8 day half-life through albumin binding; sold as research-chemical with no human therapeutic approval.
GHRP-2
Growth Hormone Releasing Peptide-2
Synthetic hexapeptide ghrelin receptor agonist stimulating GH release; clinical diagnostic in Japan, research-chemical elsewhere.
GHRP-6
Growth Hormone Releasing Peptide-6
First-generation hexapeptide ghrelin receptor agonist; pulsatile GH release with hunger stimulation, no FDA approval.
Hexarelin
Hexarelin (Examorelin)
Potent hexapeptide GH secretagogue with rapid receptor desensitization; investigated for cardiac applications in early trials.
Ipamorelin
Selective pentapeptide ghrelin receptor agonist with minimal cortisol or prolactin elevation; Phase 2 discontinued by Helsinn 2014, now compounded research chemical.
MK-677
MK-677 (Ibutamoren, Ibutamoren Mesylate)
Oral non-peptide ghrelin receptor agonist with sustained 24-hour GH elevation; Phase 2 trials completed but no FDA approval after two decades of development.
Sermorelin
Sermorelin (GRF 1-29, Geref)
N-terminal 29-amino-acid fragment of native GHRH; original FDA approval (Geref) withdrawn 2008 for commercial reasons, now compounded for off-label adult use.
Tesamorelin
TH9507
Stabilized GHRH analog. FDA-approved 2010 for HIV-associated lipodystrophy. The only GHRH analog with a complete Phase 3 file.
Growth Hormone Peptides
Growth hormone peptides are compounds that stimulate endogenous GH release rather than supplying recombinant GH directly. Two mechanism classes dominate. GHRH (growth hormone releasing hormone) analogs like Sermorelin, Tesamorelin, and CJC-1295 bind the GHRH receptor on pituitary somatotrophs and trigger pulsatile GH secretion. Ghrelin-receptor agonists like Ipamorelin, GHRP-2, GHRP-6, and Hexarelin act on a separate receptor pathway and produce a sharper, shorter GH pulse.
Tesamorelin (Egrifta) is the only compound in this class with FDA approval. It reduced visceral adipose tissue by 15 to 18 percent over 26 weeks in HIV-associated lipodystrophy across two Phase 3 trials. Sermorelin holds an older FDA approval for pediatric growth hormone deficiency. MK-677 (ibutamoren) is an orally bioavailable non-peptide ghrelin-receptor agonist with an extensive Phase 2 dataset that failed to translate IGF-1 increase into strength or function in elderly subjects.
The remaining compounds, including CJC-1295 with DAC, ipamorelin, and the GHRP family, are Research Use Only in the United States and the European Union. None has a Phase 3 efficacy file.
Doping flag. All GH secretagogues are on the World Anti-Doping Agency prohibited list under section S2. Use in competitive sport is an anti-doping rule violation.
Adverse-event signals across the class include glucose intolerance, water retention, joint pain, and IGF-1 elevation above the age-adjusted upper limit of normal. Sustained IGF-1 increase is epidemiologically associated with increased cancer risk in the general population.