GHK-Cu — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for GHK-Cu, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| Copper delivery and redox signalling | Chelate-mediated | The characterised activity is copper delivery to tissue with associated effects on gene expression |
| Metalloproteinase and collagen gene expression | Transcriptional effects | Reported across a broad set of genes in cultured fibroblasts |
§2.2Mechanism of action
GHK is a naturally occurring tripeptide present in plasma at concentrations that decline with age. Complexed with copper it acts as a physiological copper carrier and, in cultured human fibroblasts, alters expression of a broad set of genes associated with extracellular-matrix remodelling, antioxidant defence and DNA repair. Topical dermatological effects are the best-supported application. The Institute notes that gene-expression breadth in cell culture is frequently presented as though it established systemic therapeutic effect, and that it does not.[1,2]
§2.3Pharmacokinetics
No human pharmacokinetic characterisation of GHK-Cu has been identified. In the absence of a half-life, a volume of distribution and a clearance estimate, no dosing interval used in practice can be related to any exposure that produced an effect in any study, and the Institute records this as a first-order gap rather than a detail.
§2.4Interactions
- Zinc supplementation competes with copper absorption and handling
- Chelating agents would be expected to disrupt the complex
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.
- Pickart L, Margolina A. Regenerative and protective actions of the GHK-Cu peptide in the light of the new gene data. International Journal of Molecular Sciences 2018;19(7):1987. doi:10.3390/ijms19071987 · PMID 29986520
- D’Hondt M, Bracke N, Taevernier L, Gevaert B, Verbeke F, Wynendaele E, De Spiegeleer B. Related impurities in peptide medicines. Journal of Pharmaceutical and Biomedical Analysis 2014;101:2–30. doi:10.1016/j.jpba.2014.06.012 · PMID 25044089
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.