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Lexicon

KPV Oral

The anti-inflammatory tripeptide KPV as a tablet, especially sensible for the gut because it is specifically taken up there.

1 min read 8 sources

White tablet bottle with a black TPD label for KPV Oral on a white podium, next to it a molecule model of blue and white glass spheres with a ring in a bright lab
Preclinical · not approved

Summary

At a glance

Sources checked on 26 Oct 2026

Less inflammation marker
~50 %

Rise in MPO during colitis roughly halved, mice, KPV in drinking water1

More KPV in the colon
3.8 -fold

with a swallowed carrier compared with free KPV, mice5

Less substance in nanoparticles
12,000 -fold

lower concentration than in free solution with similar efficacy (mice)3

Human trials in the registry
0 trials

no trial with KPV on ClinicalTrials.gov, as of 26 Oct 20267

  • KPV Oral is the tripeptide Lys-Pro-Val as a tablet. KPV is the end piece of the body's own hormone alpha-MSH and dampens inflammation without tanning the skin.86
  • In the gut the transporter PepT1 carries small peptides into the cells. PepT1 is barely present in the healthy colon but increased in bowel inflammation. There KPV dampens the NF-κB pathway.12
  • In colitis models in mice the animals received KPV in their drinking water, so by mouth. The rise of the inflammation marker MPO was about 50 percent smaller in the DSS model.1
  • Swallowed carriers (nanoparticles, gels, new conjugates) brought more KPV into the inflamed colon and worked in mice even at smaller amounts.345
  • There is no study on the tablet itself and the registry lists no human trial with KPV (as of October 2026). Everything here is preclinical research, not a recommendation.7
Profile

Updated May 2026

Class
Anti-inflammatory tripeptide

oral

Use
Oral

tablet, 500mcg

Focus
Gut

inflammation

Status
Preclinical

mainly gut models

Sizes
250 mcg

1 size in the shop

Contents 13 sections
  1. At a glance
  2. What is KPV Oral?
  3. How it works
  4. How to take it
  5. Dosing
  6. What the research shows
  7. Research status
  8. Side effects
  9. Storage
  10. Related compounds
  11. FAQ
  12. Glossary
  13. Sources

What is KPV Oral?

KPV Oral is the tablet form of the anti-inflammatory tripeptide KPV (see lexicon entry). With KPV especially, oral use is particularly obvious: the peptide is taken up via the gut transporter PepT1, which is even upregulated during inflammation.

Comparison

KPV and other peptides for the gut

Entries with KPV or a gut focus, as described in the TPD lexicon. Tap a card to open its entry.

Simplified: KPV is taken up via PepT1. BPC-157 works differently and is not tied to a known transporter. 1

How it works

KPV dampens central inflammation signaling routes directly inside cells. In the gut it is taken up via PepT1, so inflamed tissue absorbs KPV preferentially. That makes the oral form especially sensible for inflammatory gut topics.

The mechanism in detail is in the KPV entry.

Where it acts

Where KPV acted in experiments

Tap a point or a card. Colour = target, grey = observed. All from cell and animal studies.

  1. Gut

    Uptake via PepT1, inflammation dampened in colitis models1

    PepT1NF-κB
  2. Gastrointestinal passage

    Carriers protected KPV and brought 3.8 times more into the colon5

    Observed in trials
  3. Lung

    Swallowed KPV conjugate accumulated in inflamed lungs of mice5

    Observed in trials

Known targets1

Compound PubChem CID 125672: two described targets, type of action on each card.

Peptide transporter PepT1
Gene
SLC15A1
UniProt
P46059
ChEMBL
CHEMBL4605
Action
Transporter, carries KPV into gut and immune cells
NF-κB subunit p65
Gene
RELA
UniProt
Q04206
ChEMBL
CHEMBL5533
Action
Pathway dampened, not an agonist
Glass intestinal villi, glowing red and orange on the left, cool light blue on the right, blue molecules sending points of light into both areas
KPV enters inflamed gut cells via PepT1. Symbolic image.

How to take it

Oral, usually one tablet (500mcg) per day with some water.

Closed white tablet bottle with a black TPD label for KPV Oral, a glass of water and a few white tablets beside it
Taken orally with some water. Symbolic image.

Dosing

Dosing

Dosing, titration and syringe

Loading the dosing information …

  • Getting started and stepping up, drawn as a staircase
  • Units on the U-100 syringe for every step
  • How long one vial lasts

What the research shows

A study (Dalmasso, 2008) showed that PepT1-mediated uptake of KPV markedly reduced inflammation in gut models, which is exactly what supports oral use. Large human studies are missing, KPV stays in the experimental range.

Study results

What the trials measured

Interactive: switch tabs, tap points, show or hide arms. Arms are named relative to each other, no dosing advice.

Inflammation in the gut1

How much KPV lowered the rise caused by inflammation, in percent

MPO in DSS colitis1 Mice, 8 days, 5 animals per group
Without KPV (comparison) 0%
KPV in drinking water -50%
MPO in TNBS colitis1 Mice
Without KPV (comparison) 0%
KPV in drinking water -30%

Rounded values from the results section of the study (about 50 and 30 percent). MPO is an enzyme from inflammatory cells and serves as a measure of tissue inflammation. Given in drinking water, not as a tablet, not tested in humans.

More KPV at the site of inflammation5

Accumulation in the colon compared with free KPV, mice with colitis

Swallowed conjugate5 releases KPV only during inflammation
Free KPV, swallowed 1.0-fold
KPV in a swallowed carrier 3.8-fold

Free KPV as reference (1-fold). According to the abstract the conjugate worked better even though the amount was 20-fold smaller. A single study from 2026, mice only.

Clear glass colon surrounded by sweeping light trails
The data come from cell and mouse experiments. Symbolic image.

Research status

Where the research stands

Where the compound stands on the way from lab research to approval. As of 26 Oct 2026. 7

  1. Preclinical Cell assays and mice, KPV in drinking water
  2. Phase 1 no registered trial
  3. Phase 2 no registered trial
  4. Phase 3 no registered trial
  5. Approval not yet
Not approved and no registered human trial. KPV has only been studied preclinically so far, the tablet not at all.7

So far there is no registered trial in humans. 7

Side effects

  • Generally well tolerated.
  • Solid human data are limited.

Storage

Store dry, cool and protected from light, out of reach of children. Keep the original container closed and mind the expiry date.

Three white tablet bottles and a folded light blue towel on a white shelf
Dry, cool and dark in the closed original container. Symbolic image.

Related

Related compounds

Blends with KPV Oral or a different path: all in the TPD lexicon.

FAQ

Common questions about KPV Oral

Short answers, each backed by the sources below.

Are there studies on KPV as a tablet?

No. There is no published study on the tablet. The gut studies in mice also gave KPV by mouth, though: in drinking water or in carriers that release the compound only in the colon.124

Is KPV approved or studied in humans?

No. There is no approval and as of 26 October 2026 ClinicalTrials.gov lists not a single trial with KPV. All data come from cell experiments and animal models.7

Why via the gut in particular?

The transporter PepT1 carries small peptides of two or three building blocks into cells, KPV included. PepT1 is barely present in the healthy colon but increased in chronic bowel inflammation. So KPV preferentially reaches the inflamed areas. In mice without PepT1 the effect of KPV on colon tumours after inflammation was absent.12

What do the gut models show?

With KPV in the drinking water the inflammation marker MPO fell by about 50 and 30 percent of the rise (two colitis models) and weight loss was smaller. In a model of colon cancer after inflammation fewer tumours formed, but not in a genetic tumour model without inflammation.12

What do carriers like nanoparticles add?

They protect KPV on its way through stomach and small intestine and release it in the colon. In nanoparticles a 12,000-fold lower concentration gave a similar effect. A newer conjugate brought 3.8 times more KPV into the colon and worked better even at a 20-fold smaller amount.345

Which side effects are known?

There are no solid data because KPV has never been tested in a registered human trial. The nanoparticle carriers did not damage gut cells in cell experiments. That cannot be transferred to humans.734

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

Alpha-MSH
The body's own hormone made of 13 building blocks. It controls skin tanning and dampens inflammation. KPV is its last three building blocks.
Colitis
Inflammation of the colon. In research it is triggered in mice with substances such as DSS or TNBS.
MPO
Myeloperoxidase: an enzyme from white blood cells. The more MPO in the tissue, the more inflammatory cells have moved in.
Nanoparticles
Tiny carrier particles. They protect a compound and deliver it more precisely to the site of inflammation.
NF-κB
A switch in the cell nucleus that turns on many genes for inflammatory messengers.
PepT1
Transporter in the gut cell membrane that brings small peptides of two or three building blocks into the cell. Increased in the colon during bowel inflammation.
Preclinical
Research before first use in humans, in cell cultures and animal models.
Tripeptide
A chain of exactly three amino acids. For KPV these are lysine, proline and valine.
Upregulated
The cell makes more of a protein than usual, here more PepT1 during inflammation.

Evidence

Sources

Show all 8 sourcesHide sources 6 Studies1 Trial registry1 Database checked 26 Oct 2026

Studies

  1. KPV uptake via PepT1 reduces gut inflammation (cells and mice)

    Dalmasso et al., Gastroenterology, 2008

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed, PMC (Volltext)
  2. PepT1 and KPV in drinking water in colon cancer after inflammation (mice)

    Viennois et al., Cellular and Molecular Gastroenterology and Hepatology, 2016

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed, Europe PMC (Volltext)
  3. KPV in nanoparticles against colitis (mice)

    Laroui et al., Gastroenterology, 2010

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. Swallowed KPV nanoparticles with hyaluronic acid (mice)

    Xiao et al., Molecular Therapy, 2017

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  5. Inflammation-triggered carriers for oral KPV (mice)

    Cheng et al., Science Advances, 2026

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  6. Review of alpha-MSH and related tripeptides

    Brzoska et al., Endocrine Reviews, 2008

    Checked 26 Oct 2026 via doi.org, Crossref, PubMed

Trial registry

  1. Search on ClinicalTrials.gov (no trial with KPV)

    ClinicalTrials.gov, U.S. National Library of Medicine

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. Structure of Lys-Pro-Val in PubChem

    PubChem, U.S. National Library of Medicine (CID 125672)

    Checked 26 Oct 2026 via PubChem

In the shop

KPV Oral in the catalog

Sizes, prices and shipping times are on the product page.

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