K4 Elite
K4 Elite
KPV is the C-terminal tripeptide (Lys-Pro-Val) of α-melanocyte-stimulating hormone. It has been studied in mouse and rat colitis models (oral in drinking water, and rectal or oral nanoparticle/hydrogel formulations) and in human intestinal epithelial and T-cell lines, where nanomolar concentrations reduced NF-κB activation. No human clinical trial of KPV has been published or registered; FDA's Category 2 entry states it 'has not identified any human exposure data on drug products containing KPV administered via any route'.
Each row records what a published study did: who it enrolled, the regimen it administered to those subjects, and what it reported. These are historical study descriptions, not protocols to follow.
| Study | Population | Regimen as reported | Primary findings |
|---|---|---|---|
| Dalmasso et al., Gastroenterology 2008 (mouse DSS and TNBS colitis; human cell lines; preclinical) | Mice with dextran-sulfate-sodium- or TNBS-induced colitis; Caco2-BBE and HT29-Cl.19A intestinal epithelial cells and Jurkat T cells in vitro | KPV was added to the drinking water of mice with DSS- or TNBS-induced colitis, and cultured human epithelial and T cells were exposed to KPV at nanomolar concentrations under cytokine stimulation. | Oral KPV reduced the incidence and pro-inflammatory cytokine expression of DSS- and TNBS-induced colitis in mice; in vitro, KPV uptake was PepT1-mediated and nanomolar KPV inhibited NF-κB and MAP-kinase signalling. |
| Kannengiesser et al., Inflamm Bowel Dis 2008 (mouse DSS colitis and CD45RBhi transfer colitis; preclinical) | Mice with DSS colitis, CD45RB(hi) T-cell transfer colitis, and MC1R-deficient (MC1Re/e) mice with DSS colitis | Mice with colitis were treated with the α-MSH(11-13) tripeptide KPV and monitored by body weight, colonic histology and myeloperoxidase activity. | KPV-treated mice showed earlier recovery and greater regain of body weight, reduced inflammatory infiltrates and lower colonic MPO activity; effects persisted in MC1R-deficient mice, suggesting partial independence from MC1R signalling. |
| Xiao et al., Mol Ther 2017 (mouse ulcerative colitis; oral hyaluronic-acid nanoparticles; preclinical) | Mice with experimental ulcerative colitis | KPV was loaded into hyaluronic-acid-functionalised polymeric nanoparticles (~272 nm) and delivered orally to target colonic epithelial cells and macrophages. | The authors report the nanoparticles were non-toxic and biocompatible in their assays and that oral targeted delivery of KPV alleviated colitis in mice. |
| Sun et al., ACS Biomater Sci Eng 2021 (rat TNBS colitis; rectal hydrogel; preclinical) | Rats with TNBS-induced ulcerative colitis | KPV was administered rectally in a self-cross-linked cysteamine-grafted γ-polyglutamic acid hydrogel; the authors note that KPV solution alone is unstable when given rectally. | The hydrogel formulation was developed to stabilise KPV for rectal delivery and was evaluated for attenuation of TNBS colitis in rats. |
Effects recorded in the cited reports. Frequencies are those the source reported, in the population that source studied.
| Effect | Frequency / context | Source |
|---|---|---|
| No human adverse-event data exist | FDA states it 'has not identified any human exposure data on drug products containing KPV administered via any route of administration' and 'lacks important information regarding any safety issues raised by KPV, including whether it would cause harm if administered to humans'. | FDA — Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks ↗ |
| PepT1-dependent uptake (mechanistic note from animal work) | KPV's anti-inflammatory effect in mice and cell lines depends on the PepT1 di/tripeptide transporter, which is up-regulated in inflamed colon; a 2016 mouse study from the same group reported that PepT1 overexpression promoted colitis-associated cancer while KPV was tested as a therapeutic in that model. No toxicity of KPV itself was reported in these studies. | Critical role of PepT1 in promoting colitis-associated cancer and therapeutic benefits of the anti-inflammatory PepT1-mediated tripeptide KPV in a murine model (Cell Mol Gastroenterol Hepatol 2016) ↗ |
No interactions with a verifiable citation have been indexed for this compound.
Exclusions and label contraindications recorded in the cited sources.