KPV is the three-amino-acid C-terminal fragment of alpha-melanocyte stimulating hormone. Its interest lies in the separation of functions: the parent hormone carries both potent anti-inflammatory activity and melanocortin receptor-mediated pigmentary and cardiovascular effects, whereas the KPV fragment appears to retain the former while largely losing the latter. Preclinical work, principally in murine colitis models, has demonstrated reduction in inflammatory markers and mucosal healing following both systemic and oral administration, with evidence that the peptide is taken up directly by intestinal epithelial cells. There is also an antimicrobial literature. Human clinical trials have not been conducted. PHI supplies KPV for clinician-directed use in an inflammatory or mucosal context.
Active Compound: KPV (Lys-Pro-Val, alpha-MSH 11-13)
Permitted Claim GuidelinesAn anti-inflammatory fragment of alpha-MSH studied in preclinical models of mucosal inflammation. Used under practitioner supervision. Human clinical evidence is not available.
Mechanism of ActionEnters cells directly, including intestinal epithelial cells via the PepT1 transporter, and acts intracellularly to inhibit NF-kB and MAPK inflammatory signalling cascades, reducing production of pro-inflammatory cytokines. Unlike the parent alpha-MSH molecule, this action does not appear to require melanocortin receptor binding, which accounts for the absence of pigmentary effects.
Evidence Grade: D - Preclinical evidence only; no human trials
Clinical Evidence BaseConsistent preclinical data in murine models of colitis showing reduced inflammatory markers and improved mucosal healing. In vitro antimicrobial activity reported against certain bacterial and fungal species. No published human clinical trials.
Literature & ReferencesDalmasso G et al. Gastroenterology, 2008 - PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. | Kannengiesser K et al. Inflamm Bowel Dis, 2008 - melanocortin-derived tripeptide KPV has anti-inflammatory potential. | Cutuli M et al. J Leukoc Biol, 2000 - antimicrobial effects of alpha-MSH peptides.
Safety & PrecautionsNo significant toxicity signal in animal work, but human safety data are absent and long-term risk is unknown. Immunomodulatory activity warrants caution in patients with autoimmune disease or on immunosuppressive therapy, and in active infection. Not for use in pregnancy or breastfeeding. Injection-site reactions are the most commonly reported effect.
ContraindicationsActive systemic infection; concurrent immunosuppressive therapy without specialist review; pregnancy and breastfeeding; known hypersensitivity.
Storage & HandlingStore lyophilised vial at 2-8 C, protected from light.
Regulatory StatusNot authorised as a medicine in the UK, EU or US. Supplied only through appropriate professional, prescription-led channels.