CJC-1295

Mechanism

In plain terms it tells the pituitary gland to release more of the body's own growth hormone. Technically, it binds the GHRH receptor (a Gs-coupled G-protein-coupled receptor) on anterior-pituitary somatotrophs, raising intracellular cAMP and activating protein kinase A to stimulate both synthesis and pulsatile release of endogenous growth hormone, which secondarily raises IGF-1. Four amino-acid substitutions (D-Ala2, Gln8, Ala15, Leu27) resist enzymatic degradation, and in the DAC version a lysine-linked maleimidopropionamide moiety forms a covalent bond with cysteine-34 of albumin, extending the half-life from minutes to about a week (Teichman et al., 2006).

Regulatory Status by Region

• United States (FDA)Not approved for any indication and never marketed. FDA placed CJC-1295 in Category 2 (potential significant safety risk) of the interim 503A bulk drug substances list; the nomination was later withdrawn/removed and the Pharmacy Compounding Advisory Committee did not recommend it for the 503A bulks list.
• Australia (TGA)Not on the Australian Register of Therapeutic Goods (ARTG); an unapproved GHRH analog. Supply for human therapeutic use is restricted (prescription-only class of substance) and no obesity/GH indication is approved.
• European Union (EMA)No EMA marketing authorization; not an approved medicine in the EU.
• WADAProhibited at all times under Section S2 (Peptide Hormones, Growth Factors, Related Substances and Mimetics); GHRH analogues including CJC-1295 are explicitly listed.

Key Studies

• 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 (Teichman SL, Neale A, Lawrence B, et al. J Clin Endocrinol Metab. 2006;91(3):799-805. PMID 16352683)
• Once-daily administration of CJC-1295, a long-acting GHRH analog, normalizes growth in the GHRH knockout mouse (Alba M, Fintini D, Sagazio A, et al. Am J Physiol Endocrinol Metab. 2006 (preclinical). PMID 16822960)