Kpv: Safety Profile & Research Summary
26 PubMed CitationsExpert ReviewedGMP CertifiedLast Reviewed: February 2026
Preclinical Research Summary
Key Preclinical Studies
| Study | Model | Key Findings | Ref |
|---|---|---|---|
| Dalmasso et al. (2008) | C57BL/6 mice — DSS + TNBS colitis | 100 µM KPV oral: MPO reduced ~50% (DSS); weight loss 5–10% vs 15–20% control (p < 0.05); PepT1-mediated uptake confirmed | [3] |
| Kannengiesser et al. (2008) | Mice — DSS + MC1R-KO | KPV rescued MC1Re/e mice from death in DSS colitis → mechanism is MC1R-independent | [15] |
| Xiao et al. (2017) | FVB mice — HA-KPV-NPs oral | 16 µg/kg/day × 6 days: 12,000-fold lower dose vs free KPV with equivalent efficacy; MPO to healthy-control levels (p < 0.01) | [6] |
| Viennois et al. (2016) | WT/PepT1-KO mice — AOM/DSS | KPV prevented colitis-associated cancer in WT but NOT PepT1-KO → PepT1 dependence confirmed for anti-tumorigenic effects | [23] |
| Bonfiglio et al. (2006) | Rabbits — corneal wounds | Topical KPV 4x daily × 4 days: significantly smaller corneal wounds vs control | [17] |
| Shao et al. (2022) | Rats — oral mucositis + MRSA | KPV@PPP_E hydrogel: ↓ IL-1β, TNF-α; ↑ IL-10; restored gingival tissue morphology; dual anti-inflammatory + antibacterial | [18] |
Human Data (Patent Case Studies)
| Case | n= | Result | Ref |
|---|---|---|---|
| Psoriasis (US 6,894,028) | 1 | 1 mg topical KPV: symptom relief >8 hours/application (vs 3 hours hydrocortisone); no AEs (hydrocortisone → telangiectasia/atrophy) | [9] |
| Contact Dermatitis (US 6,894,028) | 1 | Topical KPV: marked improvement within minutes; symptoms did not return | [9] |
Dose-Response Parameters
| Parameter | Value | Ref |
|---|---|---|
| Anti-inflammatory IC (NF-κB/MAPK) | 10 nM | [3] |
| Antimicrobial range | Picomolar to micromolar | [19] |
| PepT1 Km (intestinal cells) | ~160 µM | [3] |
| PepT1 Km (T-cells) | ~700 µM | [4] |
| Oral dose (murine colitis) | 100 µM in drinking water | [3] |
| HA-NP dose (12,000x potency) | 16 µg/kg/day oral | [6] |
| Plasma half-life | <30 minutes | [25] |
| Acute toxicity (LD50) | Not identified (>100 mg/kg) | [25] |
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References
- Sikiric P, et al. A new gastric juice peptide, BPC. An overview of the stomach-stress-organoprotection hypothesis. Journal of Physiology-Paris. 1993;87(5):313-327.
- Brzoska T, Luger TA, Maaser C, Abels C, Böhm M. Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives. Endocrine Reviews. 2008;29(5):581-602.
- Dalmasso G, Charrier-Hisamuddin L, Nguyen HTT, Yan Y, Sitaraman S, Merlin D. PepT1-Mediated Tripeptide KPV Uptake Reduces Intestinal Inflammation. Gastroenterology. 2008;134(1):166-178.
- Laroui H, Dalmasso G, Nguyen HT, Yan Y, Sitaraman SV, Merlin D. Drug-loaded nanoparticles targeted to the colon with polysaccharide hydrogel reduce colitis in a mouse model. Gastroenterology. 2010;138:843-853.
- U.S. Food and Drug Administration. Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks. FDA.gov. Updated 2023.
- Xiao B, Xu Z, Viennois E, Zhang Y, Zhang Z, Zhang M, Han MK, Kang Y, Merlin D. Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis. Molecular Therapy. 2017;25(7):1628-1640.
- Hiltz ME, Lipton JM. Antiinflammatory activity of a COOH-terminal fragment of the neuropeptide alpha-MSH. FASEB Journal. 1989;3:2282-2284.
- Luger TA, Brzoska T. α-MSH related peptides: a new class of anti-inflammatory and immunomodulating drugs. Annals of the Rheumatic Diseases. 2007;66(Suppl 3):iii52-iii55.
- Lipton JM, Catania AP. Use of KPV tripeptide for dermatological disorders. U.S. Patent No. 6,894,028 B2. 2005.
- Getting SJ, Schiöth HB, Perretti M. Dissection of the anti-inflammatory effect of the core and C-terminal (KPV) alpha-melanocyte-stimulating hormone peptides. Journal of Pharmacology and Experimental Therapeutics. 2003;306(2):631-637.
- Kelly JM, Moir AJG, Carlson KE, Haycock JW. Immobilized alpha-melanocyte stimulating hormone 10-13 (GKPV) inhibits tumor necrosis factor-alpha stimulated NF-kappaB activity. Peptides. 2006;27(3):431-437.
- Land SC. Inhibition of cellular and systemic inflammation cues in human bronchial epithelial cells by melanocortin-related peptides. International Journal of Physiology, Pathophysiology and Pharmacology. 2012;4(2):59-73.
- Elliott RJ, Szabo M, Wagner MJ, Kemp EH, MacNeil S, Haycock JW. alpha-Melanocyte-stimulating hormone, MSH 11-13 KPV and adrenocorticotropic hormone signalling in human keratinocyte cells. Journal of Investigative Dermatology. 2004;122(4):1010-1019.
- Songok AC, Panta P, Doerrler WT, Macnaughtan MA, Taylor CM. Structural modification of the tripeptide KPV by reductive glycoalkylation of the lysine residue. PLOS One. 2018;13(6):e0199686.
- Kannengiesser K, Maaser C, Heidemann J, 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.
- Böhm M, Luger T. Are melanocortin peptides future therapeutics for cutaneous wound healing? Experimental Dermatology. 2019;28:219-224.
- Bonfiglio V, et al. Effects of the COOH-terminal tripeptide alpha-MSH(11-13) on corneal epithelial wound healing: role of nitric oxide. Experimental Eye Research. 2006;83(6):1366-1372.
- Shao W, Chen R, Lin G, Ran K, Zhang Y, Yang J, Xu H. In situ mucoadhesive hydrogel capturing tripeptide KPV: the anti-inflammatory, antibacterial and repairing effect on chemotherapy-induced oral mucositis. Biomaterials Science. 2022;10:227-242.
- Cutuli M, Cristiani S, Lipton JM, Catania A. Antimicrobial effects of alpha-MSH peptides. Journal of Leukocyte Biology. 2000;67(2):233-239.
- Catania A, et al. Three-dimensional structure of the α-MSH-derived candidacidal peptide [Ac-CKPV]2. The Journal of Peptide Research. 2005;66(1):19-26.
- Charnley M, Moir AJG, Douglas CWI, Haycock JW. Anti-microbial action of melanocortin peptides and identification of a novel X-Pro-d/l-Val sequence in Gram-positive and Gram-negative bacteria. Peptides. 2008;29(6):1004-1009.
- Land SC, et al. KPV inhibits MMP-9 activity and reduces eotaxin and IL-8 secretion in bronchial epithelial cells. International Journal of Physiology, Pathophysiology and Pharmacology. 2012;4(2):59-73.
- Viennois E, et al. Critical Role of PepT1 in Promoting Colitis-Associated Cancer and Therapeutic Benefits of the Anti-inflammatory PepT1-Mediated Tripeptide KPV in a Murine Model. Cellular and Molecular Gastroenterology and Hepatology. 2016;2(3):340-357.
- Wu Y, et al. KPV and RAPA Self-Assembled into Carrier-Free Nanodrugs for Vascular Calcification Therapy. Advanced Healthcare Materials. 2024.
- Catania A, et al. Inhibitory effects of the peptide (CKPV)2 on endotoxin-induced host reactions. The Journal of Surgical Research. 2006;131.
- Pawar K, Kolli CS, Rangari NS, Babu RJ. Transdermal Iontophoretic Delivery of Lysine-Proline-Valine (KPV) Peptide Across Microporated Human Skin. Journal of Pharmaceutical Sciences. 2017;106(7):1814-1820.
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