KPV

Overview

KPV is the C-terminal tripeptide of alpha-melanocyte-stimulating hormone (alpha-MSH), corresponding to residues 11-13. It is the smallest alpha-MSH fragment shown to retain anti-inflammatory activity. Research-only; not FDA-approved; evidence is primarily preclinical.

Mechanism of Action

KPV enters cells (partly via the di/tripeptide transporter PepT1 in intestinal epithelium and immune cells) and acts intracellularly to inhibit NF-kB activation, decreasing production of pro-inflammatory cytokines. The anti-inflammatory effect is receptor-independent with respect to melanocortin receptors, distinguishing KPV from pigmentation-inducing MC1R agonists.

Research Summary

All in vivo evidence is preclinical. Dalmasso et al. (Gastroenterology 2008) demonstrated PepT1-mediated uptake and reduction of DSS/TNBS colitis in mice. Kannengiesser et al. (Inflammatory Bowel Diseases 2008) showed anti-inflammatory effects in two murine colitis models. Additional preclinical work (largely from the Merlin group at Georgia State) explores nanoparticle/conjugate oral delivery for IBD, and models of atopic dermatitis, asthma, and wound healing show activity. No controlled human trials have been published.

Dosing Information

Reported Side Effects

• Generally well-tolerated in limited reports
• Injection site irritation (SubQ)
• Mild GI discomfort (oral)
• Theoretical immunosuppression risk at high sustained doses (NF-kB inhibition)
• Human safety data are very limited

Labs to monitor before & during your KPV protocol

These biomarkers are commonly tracked to assess response and safety. Run baseline labs before starting, mid-cycle labs halfway through, and post-cycle labs 1–2 weeks after the final dose.

Commonly Stacked With

Research References

• Dalmasso G, et al. PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. Gastroenterology. 2008;134(1):166-178. (PMID 18061177)
• Kannengiesser K, et al. Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease. Inflammatory Bowel Diseases. 2008;14(3):324-331. (PMID 18092346)
• Brzoska T, et al. Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo. Endocrine Reviews. 2008;29(5):581-602. (PMID 18612139)