GH Secretagogues (Ipamorelin, CJC-1295, Tesamorelin) — References

Mirrored Reference Dossier

Parent Topic: GH Secretagogues (Ipamorelin, CJC-1295, Tesamorelin) | References Hub: 02 - Compounds & Molecules References MOC

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Landmark Peer-Reviewed Studies

1. Falutz et al. (2007) — New England Journal of Medicine & (2010) — Journal of Clinical Endocrinology & Metabolism

• Citation: Falutz, J., Allas, S., Blot, K., Potvin, D., Kotler, D., Somero, M., Berger, D., Brown, S., Richmond, G., Fessel, J., Turner, R., & Grinspoon, S. (2007). Metabolic effects of a growth hormone-releasing factor in patients with HIV. New England Journal of Medicine, 357(23), 2359–2370. (And pooled Phase 3 analysis: JCEM, 2010, 95(9), 4291–4304).
• Identifiers: PMID: 18057338 (PubMed · Europe PMC) (NEJM) | DOI: 10.1056/NEJMoa072375 (DOI · SciDB · Scholar) | PMID: 20554713 (PubMed · Europe PMC) (JCEM) | DOI: 10.1210/jc.2010-0490 (DOI · SciDB · Scholar)
• Study Design & Sample Size: Multicenter, randomized, double-blind, placebo-controlled Phase 3 trials ($N=412$ in NEJM; $N=816$ in pooled JCEM analysis) over 26–52 weeks evaluating $2\text{ mg/day}$ SubQ Tesamorelin.
• Key Quantitative Outcomes: Tesamorelin ($2\text{ mg/day}$) reduced L4–L5 Visceral Adipose Tissue (VAT) cross-sectional area by $-15.2\%$ at 26 weeks (vs. $+5.0\%$ in placebo; net difference $-20.2\%,p<0.001$) and $-18\%$ over 52 weeks, increased serum IGF-1 by $+81\%$ ($+109\text{ ng/mL},p<0.001$), reduced triglycerides by $-50\text{ mg/dL}$ ($p<0.001$), and improved the total cholesterol to HDL ratio without reducing beneficial limb subcutaneous adipose tissue.

2. Raun et al. (1998) — European Journal of Endocrinology

• Citation: Raun, K., Hansen, B. S., Johansen, N. L., Thøgersen, H., Madsen, K., Ankersen, M., & Andersen, P. H. (1998). Ipamorelin, the first selective growth hormone secretagogue. European Journal of Endocrinology, 139(5), 552–561.
• Identifiers: PMID: 9849822 (PubMed · Europe PMC) | DOI: 10.1530/eje.0.1390552 (DOI · SciDB · Scholar)
• Study Design & Sample Size: Foundational receptor binding, pituitary cell culture, and comparative in vivo endocrine study in rats and swine comparing Ipamorelin against GHRP-2, GHRP-6, and GHRH.
• Key Quantitative Outcomes: Ipamorelin stimulated GH release with high potency (${\text{EC}}_{50}=1.3\text{ nmol/L}$ in vitro; ${\text{ED}}_{50}=80\text{ nmol/kg}$ in vivo), comparable to GHRP-6. Crucially, while GHRP-2 and GHRP-6 caused marked surges in plasma ACTH and cortisol (equivalent to CRH stimulation), Ipamorelin produced zero elevation in plasma ACTH, cortisol, prolactin, FSH, LH, or TSH even at doses exceeding $200\times$ its ${\text{ED}}_{50}$.

3. Baker et al. (2012) — Archives of Neurology (JAMA Neurology)

• Citation: Baker, L. D., Barsness, S. M., Borson, S., Merriam, G. R., Friedman, S. D., Craft, S., & Vitiello, M. V. (2012). Effects of growth hormone–releasing hormone on cognitive function in adults with mild cognitive impairment and healthy older adults: results of a controlled trial. Archives of Neurology, 69(11), 1420–1429.
• Identifiers: PMID: 22869065 (PubMed · Europe PMC) | PMCID: PMC3600841 (PMC Full Text) | DOI: 10.1001/archneurol.2012.1970 (DOI · SciDB · Scholar)
• Study Design & Sample Size: 20-week randomized, double-blind, placebo-controlled parallel-group trial in adults aged 55–87 years ($N=152$, including healthy older adults and patients with amnestic Mild Cognitive Impairment) receiving $1.0\text{ mg/day}$ SubQ Tesamorelin ($30\text{ min}$ before bedtime).
• Key Quantitative Outcomes: Tesamorelin increased physiological IGF-1 by $+117\%$ (remaining within normal young-adult physiological bounds) and significantly improved Executive Function ($p=0.005$) and Verbal Memory ($p=0.03$), yielding an overall composite cognitive advantage ($p=0.003$) in both healthy older adults and MCI participants, while reducing body fat by $-7.4\%$ ($p<0.001$).

4. Teichman et al. (2006) — Journal of Clinical Endocrinology & Metabolism

• Citation: Teichman, S. L., Neale, A., Lawrence, B., Gagnon, C., Castaigne, J. P., & Frohman, L. A. (2006). Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. The Journal of Clinical Endocrinology & Metabolism, 91(3), 799–805.
• Identifiers: PMID: 16352683 (PubMed · Europe PMC) | DOI: 10.1210/jc.2005-1536 (DOI · SciDB · Scholar)
• Study Design & Sample Size: Two randomized, placebo-controlled, double-blind, ascending-dose Phase I/II trials in healthy adults aged 21–61 years ($N=74$).
• Key Quantitative Outcomes: Subcutaneous administration of CJC-1295 ($30\text{–}60\mu \text{g/kg}$) produced dose-dependent increases in mean plasma GH concentrations by $2\text{- to }10\text{-fold}$ for 6 days or more and increased mean plasma IGF-1 levels by $1.5\text{- to }3\text{-fold}$ for 9–11 days while preserving pulsatile GH secretion patterns.