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documented protocols

KPV: what is documented about dosing

What published work gave, in which species and by which route, reported as a record rather than as a protocol.

Last Reviewed Editorial policy Methodology

Published work on KPV records what was given to mice, rats, rabbits and cultured cells, in the model each study built. That record is set out below with the species and the route named on every line.

No study has established an amount for a person, on any route. The figures that circulate in community write-ups and on vendor pages are extrapolations from animal work or have no traceable origin, and this page does not republish them.

What this page does instead is name the source class on every figure it carries and state what that figure actually was: a culture concentration, a solution strength for a rabbit eye, or a formulation loading. None of those converts into a human amount.

Not medical advice

This page reports what has been documented about a compound. It is not medical advice, not a diagnosis, not a dosing protocol, and not a recommendation to obtain or use anything described here. Talk to a licensed clinician about anything concerning your health. Read the full disclaimer.

Reviewed against editorial standards Updated

What this page reports, and what it does not

We report what has been documented. We do not prescribe what should be done.

Nothing here is a dosing recommendation. Statements about dosing reflect community and research reports only.

No trial established an amount of KPV for a person. Most of the rows below record what a published study gave to its animals or its cells, in the model that study built, with the species and the route named on the line. One row records that other figures circulate in community write-ups, and that this site does not republish them. Nothing here is a protocol, nothing here is scaled for a person, and this site publishes no preparation steps, no administration technique and no equipment. The reasoning is in the editorial policy.

Commonly cited protocols (extrapolated, not validated)

What published studies gave, in which species and by which route, and what circulates elsewhere. The source class is named on every row, and none of it is a clinical protocol
StudyWhat was givenFrequencyDurationNotes
Mouse colitis, by mouth. Dalmasso 2008 [7]Free peptide in the animals' drinking water, at the concentration reported for that modelContinuous, for as long as the animals drankThrough the induced colitis periodThe only study that gave free KPV by mouth without a carrier. A mouse, a chemical colitis, and an intake per animal that nobody controlled
Mouse colitis, free peptide. Kannengiesser 2008 [8]Free peptide, at the amount reported for that modelPer the study protocolThrough the induced colitis period in two models, DSS and T cell transferThe second and last study to give free KPV without a carrier. Every colitis paper after 2008 built one
Rat colitis, rectal, in a hydrogel. Sun 2021 [12]Held in a self-crosslinked hydrogel, for the stability reason given in the pharmacokinetics sectionPer the study protocolThrough the TNBS colitis periodThe carrier is the point of the paper. Free KPV was the comparison arm and it did worse
Rabbit cornea, topical drops. Bonfiglio 2006 [15]1, 5 and 10 mg per millilitre in solution, 30 microlitres per dropRepeated drops through the treatment periodFour daysA rabbit eye with the epithelium mechanically removed. Nobody sells KPV for eyes
Human keratinocytes and 3D skin, in culture. Sung 2025 [20]50 micrograms per millilitre in the culture mediumSingle treatment around the particulate challengePer the assayCells in a dish. A culture concentration is not a dose and does not convert into one
Rodent colitis, in nanoparticles, hydrogels or a prodrug. Laroui 2010, Xiao 2017, Zhao 2022, Cheng 2026 [9] [11] [13] [14]Loaded into the carrier. The free peptide amount is set by the formulation, not chosen independentlyPer each study protocolDays to weeks, depending on the modelFive of the seven rodent colitis studies delivered KPV inside something engineered. None of those carriers is what is sold
Community write-ups and vendor pagesFigures circulate. This site does not republish themFigures circulateFigures circulateNo trial established an amount for a person, so any figure in circulation is an extrapolation from a rodent or has no origin at all. Republishing one would supply an instruction with a hedge around it, which is the thing this site exists not to do

One thing in that table is worth pulling out: the marketed presentation, a lyophilised powder in a vial, has never been studied in any animal, let alone a person.

The second is that a concentration in a culture dish and a concentration in a rodent's drinking water are not doses and do not convert into one. Body-weight scaling between species is unreliable even between two mammals given the same route, and none of these studies used the route the compound is sold for.

Our takeThe most useful sentence anyone can write about KPV amounts is that the marketed presentation has never been studied in an animal, never mind a person. Everything else in this area is arithmetic stacked on an assumption.

Main routes people compare

Gut-directed: oral and rectal

Published animal studies used gut-directed delivery more often than any other route. The mechanism work offers a reason researchers chose it: PepT1 sits in the lining of the intestine and pulls tripeptides in. One study gave free KPV in mouse drinking water [7]. The others built delivery systems: hyaluronic-acid-functionalised nanoparticles [11], a self-crosslinked hydrogel for rectal administration in rats [12], a mucoadhesive double-network hydrogel that binds preferentially to inflamed mucosa [13], and a prodrug that releases KPV only where reactive oxygen species are elevated [14].

The 2026 prodrug paper is the clearest statement of the problem all of those exist to solve: the conjugate reached 3.8 times the colonic accumulation of free KPV and held its effect at a twentyfold lower amount. That is a measurement of how poorly free KPV arrives [14]. [Animal] [7] [11] [12] [13] [14]

Topical

This is the route the 2015 compounding nomination asked for, at 0.1 percent in a cream or gel, and it is the route with the clearest laboratory obstacle. Passive permeation of KPV across dermatomed human cadaver skin fell below the assay limit of detection [17]. Microneedle pretreatment, iontophoresis, and the two combined raised it, which is a finding about those techniques rather than about a cream.

Cell work on human keratinocytes is a separate question and does not answer this one: it puts KPV directly onto cells at a concentration the experimenter chose [20]. Getting there through intact skin is the step nobody has shown. [In-vitro] [17] [20]

Systemic

The two general anti-inflammatory mouse studies gave KPV systemically, in an ear swelling model and in two peritonitis models [1] [2]. Neither used the route community sources discuss, neither was in a person, and no pharmacokinetic measurement exists for any systemic route in any species.

This site publishes no preparation procedure, no administration technique and no equipment, on any route. The reasoning is set out in the editorial policy. [Animal] [1] [2]

What is said about cycle length and timing

Cycle lengths, loading phases and washout periods circulate widely for KPV. None of them came from a study, because no study has run long enough in anything to define one. The rodent colitis experiments ran for the length of the induced injury, which is days to a few weeks. The rabbit corneal study ran four days.

Timing claims, with food or without, morning or evening, have the same status. No pharmacokinetic study in any species exists that could support or contradict them.

Where a figure has a source, this page names it. Where it does not, this page says so rather than repeating it with a disclaimer attached.

Talk to a licensed clinician about anything concerning your health.

Frequently asked questions

Is there a documented KPV dose?

Not for a person, on any route. No trial has ever been run, so nothing established an amount. What is documented is what individual studies gave to mice, rats, rabbits or cultured cells, and those figures are properties of those experiments rather than starting points for anything else.

Why does this page not list the figures that appear on vendor sites?

Because none of them traces to a study in a person, and publishing one with a hedge attached still supplies an instruction. This site links to storefronts under common ownership, which makes anything published here readable as labelling for what those storefronts sell, so the rule is stricter here than at an independent publisher. The reasoning is on the editorial policy page.

Which route has the most published work behind it?

Gut-directed, by a wide margin: seven rodent colitis studies used oral or rectal delivery. The mechanism work offers a reason researchers chose it, in that the PepT1 transporter that carries KPV into cells sits in the lining of the intestine. Five of those seven delivered KPV inside an engineered carrier rather than as free peptide, so the route with the most work behind it is also the one where the free peptide performed worst.

Does this site publish preparation steps?

No. No preparation procedure, no administration technique and no equipment appears anywhere on this site, for any compound. That is a standing rule rather than a judgement about KPV, and the reasoning is on the editorial policy page.

How long did the animal studies run?

Days to a few weeks. The rodent colitis experiments ran for the length of the induced injury, and the rabbit corneal study ran four days. No study in any species has run long enough to say anything about extended exposure.

Is oral KPV absorbed?

In rodents, PepT1 carries it into the cells lining the intestine, and that transport step is well demonstrated in cells and in mice. How much survives to get there is the open question: a 2026 paper reports a prodrug conjugate reaching 3.8 times the colonic accumulation of free KPV, which is a direct measurement of how poorly the free peptide arrives. Nothing equivalent has been measured in a person.

References

  1. Hiltz ME, Lipton JM. Antiinflammatory activity of a COOH-terminal fragment of the neuropeptide alpha-MSH. FASEB J. 1989. PMID 2550304
  2. Getting SJ, Schioth HB, Perretti M. Dissection of the anti-inflammatory effect of the core and C-terminal (KPV) alpha-melanocyte-stimulating hormone peptides. J Pharmacol Exp Ther. 2003. PMID 12750433 DOI 10.1124/jpet.103.051623
  3. Mandrika I, Muceniece R, Wikberg JE. Effects of melanocortin peptides on lipopolysaccharide/interferon-gamma-induced NF-kappaB DNA binding and nitric oxide production in macrophage-like RAW 264.7 cells: evidence for dual mechanisms of action. Biochem Pharmacol. 2001. PMID 11239505 DOI 10.1016/s0006-2952(00)00583-9
  4. Lyson K, Ceriani G, Takashima A, Catania A, Lipton JM. Binding of anti-inflammatory alpha-melanocyte-stimulating-hormone peptides and proinflammatory cytokines to receptors on melanoma cells. Neuroimmunomodulation. 1994. PMID 7489322 DOI 10.1159/000097145
  5. 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. J Invest Dermatol. 2004. PMID 15102092 DOI 10.1111/j.0022-202X.2004.22404.x
  6. Land SC. Inhibition of cellular and systemic inflammation cues in human bronchial epithelial cells by melanocortin-related peptides: mechanism of KPV action and a role for MC3R agonists. Int J Physiol Pathophysiol Pharmacol. 2012. PMID 22837805
  7. Dalmasso G, Charrier-Hisamuddin L, Nguyen HT, Yan Y, Sitaraman S, Merlin D. PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. Gastroenterology. 2008. PMID 18061177 DOI 10.1053/j.gastro.2007.10.026
  8. Kannengiesser K, Maaser C, Heidemann J, Luegering A, Ross M, Brzoska T, Bohm M, Luger TA, Domschke W, Kucharzik T. Melanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease. Inflamm Bowel Dis. 2008. PMID 18092346 DOI 10.1002/ibd.20334
  9. 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. PMID 19909746 DOI 10.1053/j.gastro.2009.11.003
  10. Viennois E, Ingersoll SA, Ayyadurai S, Zhao Y, Wang L, Zhang M, Han MK, Garg P, Xiao B, Merlin D. 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. PMID 27458604 DOI 10.1016/j.jcmgh.2016.01.006
  11. 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. Mol Ther. 2017. PMID 28143741 DOI 10.1016/j.ymthe.2016.11.020
  12. Sun J, Xue P, Liu J, Huang L, Lin G, Ran K, Yang J, Lu C, Zhao YZ, Xu HL. Self-cross-linked hydrogel of cysteamine-grafted gamma-polyglutamic acid stabilized tripeptide KPV for alleviating TNBS-induced ulcerative colitis in rats. ACS Biomater Sci Eng. 2021. PMID 34547895 DOI 10.1021/acsbiomaterials.1c00792
  13. Zhao Y, Xue P, Lin G, Tong M, Yang J, Zhang Y, Ran K, Zhuge D, Yao Q, Xu H. A KPV-binding double-network hydrogel restores gut mucosal barrier in an inflamed colon. Acta Biomater. 2022. PMID 35245681 DOI 10.1016/j.actbio.2022.02.039
  14. Cheng J, Wu P, Li C, Han Y, Sun M, Dou Y, Chen S, Zhang J. Inflammation-triggered self-immolative conjugates enable oral peptide delivery by overcoming gastrointestinal barriers. Sci Adv. 2026. PMID 41533788 DOI 10.1126/sciadv.aea2989
  15. Bonfiglio V, Camillieri G, Avitabile T, Leggio GM, Drago F. Effects of the COOH-terminal tripeptide alpha-MSH(11-13) on corneal epithelial wound healing: role of nitric oxide. Exp Eye Res. 2006. PMID 16965771 DOI 10.1016/j.exer.2006.07.014
  16. Pawar KR, Mulabagal V, Smith F, Kolli CS, Rangari VK, Babu RJ. Stability-indicating HPLC assay for lysine-proline-valine (KPV) in aqueous solutions and skin homogenates. Biomed Chromatogr. 2015. PMID 25298219 DOI 10.1002/bmc.3347
  17. Pawar K, Kolli CS, Rangari VK, Babu RJ. Transdermal iontophoretic delivery of lysine-proline-valine (KPV) peptide across microporated human skin. J Pharm Sci. 2017. PMID 28343991 DOI 10.1016/j.xphs.2017.03.017
  18. 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. PMID 29953505 DOI 10.1371/journal.pone.0199686
  19. Zhao Y, Huang L, Lin G, Tong M, Xie Y, Pan H, Shangguan J, Yao Q, Xu S, Xu H. Skin-adaptive film dressing with smart-release of growth factors accelerated diabetic wound healing. Int J Biol Macromol. 2022. PMID 36240893 DOI 10.1016/j.ijbiomac.2022.10.054
  20. Sung J, Ju SY, Park S, Jung WK, Je JY, Lee SJ. Lysine-Proline-Valine peptide mitigates fine dust-induced keratinocyte apoptosis and inflammation by regulating oxidative stress and modulating the MAPK/NF-kappaB pathway. Tissue Cell. 2025. PMID 40073467 DOI 10.1016/j.tice.2025.102837
  21. Brzoska T, Luger TA, Maaser C, Abels C, Bohm M. Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives for the treatment of immune-mediated inflammatory diseases. Endocr Rev. 2008. PMID 18612139 DOI 10.1210/er.2007-0027
  22. Brzoska T, Bohm M, Lugering A, Loser K, Luger TA. Terminal signal: anti-inflammatory effects of alpha-melanocyte-stimulating hormone related peptides beyond the pharmacophore. Adv Exp Med Biol. 2010. PMID 21222263 DOI 10.1007/978-1-4419-6354-3_8
  23. Bohm M, Luger T. Are melanocortin peptides future therapeutics for cutaneous wound healing? Exp Dermatol. 2019. PMID 30661264 DOI 10.1111/exd.13887
  24. Gravina AG, Pellegrino R, Durante T, Palladino G, Imperio G, D'Amico G, Trotta MC, Dallio M, Romeo M, D'Amico M, Federico A. The melanocortin system in inflammatory bowel diseases: insights into its mechanisms and therapeutic potentials. Cells. 2023. PMID 37508552 DOI 10.3390/cells12141889
  25. US Food and Drug Administration. KPV-related bulk drug substances: briefing document for the Pharmacy Compounding Advisory Committee, review dated 12 May 2026. FDA advisory committee materials. 2026. Source document
  26. US Food and Drug Administration. Questions for PCAC regarding whether FDA should include certain bulk drug substances on the 503A Bulks List, Pharmacy Compounding Advisory Committee, 23 and 24 July 2026. Distributed as the final questions file; its own internal headers read QUESTIONS and DRAFT QUESTIONS (cont.). FDA advisory committee materials. 2026. Source document
  27. US Food and Drug Administration. Pharmacy Compounding Advisory Committee; notice of meeting; establishment of a public docket; request for comments. Docket No. FDA-2025-N-6895. Federal Register, document 2026-07361. 2026. Source document
  28. World Anti-Doping Agency. The 2026 Prohibited List, international standard, effective 1 January 2026. WADA. 2026. Source document
  29. Sun MC, Xu XL, Du Y, Lou XF, Wang W, You YC, Liu D, Jin FY, Qi J, Zhu MX, Zhu LW, Wang J, Du YZ. Biomimetic Melanosomes Promote Orientation-Selective Delivery and Melanocyte Pigmentation in the H2O2-Induced Vitiligo Mouse Model. ACS Nano. 2021. PMID 34662120 DOI 10.1021/acsnano.1c05321
  30. US Department of Defense, Operation Supplement Safety. Ingredient and substance index, and the DoD prohibited dietary supplement ingredients list. Checked for a KPV entry on 2 August 2026; BPC-157 appears, KPV does not. OPSS, Uniformed Services University. 2026. Source document
  31. Cutuli M, Cristiani S, Lipton JM, Catania A. Antimicrobial effects of alpha-MSH peptides. J Leukoc Biol. 2000. PMID 10670585 DOI 10.1002/jlb.67.2.233
  32. Böhm M, Apel M, Sugawara K, Brehler R, Jurk K, Luger TA, Haas H, Paus R, Eiz-Vesper B, Walls AF, Ponimaskin E, Gehring M, Kapp A, Raap U. Modulation of basophil activity: a novel function of the neuropeptide alpha-melanocyte-stimulating hormone. J Allergy Clin Immunol. 2012. PMID 22178636 DOI 10.1016/j.jaci.2011.11.012