CJC-1295 — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for CJC-1295, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| GHRH receptor (GHRHR) | Agonist | Four substitutions (D-Ala2, Gln8, Ala15, Leu27) confer resistance to DPP-4 and to enzymatic and chemical degradation |
| Albumin Cys34 (DAC variant only) | Covalent conjugation | Irreversible thioether bond; the basis of the multi-day half-life |
§2.2Mechanism of action
Both variants are GHRH receptor agonists that increase pulsatile growth-hormone secretion and, downstream, IGF-1. The DAC variant achieves sustained exposure by covalently bonding to albumin in vivo, producing a continuous rather than pulsatile GHRH signal. Whether continuous GHRH receptor stimulation preserves the physiological pulsatility of growth-hormone release is a substantive mechanistic question that the available human data do not answer.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- ≈30 min (modified GRF(1-29)); ≈5.8–8.1 days (DAC variant)
- Time to maximum concentration
- not reliably published
- Volume of distribution
- not published
- Plasma protein binding
- covalently bound to albumin (DAC variant)
- Clearance
- not published
- Bioavailability
- not published
The DAC variant is eliminated with albumin turnover. The non-DAC variant is cleaved proteolytically.
§2.4Interactions
- Not characterised
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- Teichman SL, Neale A, Lawrence B, Gagnon C, Castaigne JP, Frohman LA. 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. Journal of Clinical Endocrinology & Metabolism 2006;91(3):799–805. doi:10.1210/jc.2005-1536 · PMID 16352683
- Prakash A, Goa KL. Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs 1999;12(2):139–157. doi:10.2165/00063030-199912020-00007 · PMID 18031173
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.