- subcutaneous
- oral
- topical
KPV
Lysine-Proline-Valine (α-MSH C-terminal tripeptide)
KPV at a glance
Nomination withdrawnHow studies gave it
Injected into the fat under the skin, or swallowed, or applied to the skin
Evidence on this page
6 peer-reviewed papers, published 1989 to 2017
FDA compounding lists
It was nominated for compounding use and the nomination was withdrawn.
What it is
A 3-amino-acid linear tripeptide corresponding to residues 11–13 at the C-terminus of alpha-melanocyte-stimulating hormone (α-MSH). KPV retains the anti-inflammatory activity studied in α-MSH research without the melanogenic (skin-darkening) effects. Its anti-inflammatory properties were first described by Hiltz and Lipton in 1989.
Preclinical studies have examined its mechanism as an NF-κB inhibitor transported into intestinal cells via the PepT1 (SLC15A1) transporter, which is upregulated in IBD models. No human clinical trials have been conducted for KPV itself.
Published research
Anti-inflammatory properties first described by Hiltz and Lipton (FASEB J 1989). Dalmasso et al. (Gastroenterology 2008) demonstrated intestinal anti-inflammatory effect is PepT1-mediated, not melanocortin receptor-mediated. Land (2012) showed KPV enters the cell nucleus and blocks NF-κB nuclear translocation by interfering with importin-α3 binding on the p65/RelA subunit.
Getting et al. (2003) confirmed effects persisted in MC1R-deficient mice. Studied in DSS-induced colitis, TNBS-induced colitis, and colitis-associated cancer models. Xiao et al. (Mol Ther 2017) developed HA-PLGA nanoparticles for oral targeted delivery with improved efficacy in colitis models. A structurally related derivative K(D)PT has undergone a clinical trial in ulcerative colitis, but KPV itself has not entered human testing.
Community-discussed routes include subcutaneous (200–500 mcg/day), oral (500–1,500 mcg/day for gut-targeted use), and topical (0.005–0.1% cream).
What the terms on this page mean8 termsHide
- tripeptide
- A peptide three amino acids long. Pentapeptide means five, and so on.
- MSH
- Melanocyte-stimulating hormone, involved in skin pigment and in appetite signalling.
- preclinical
- Laboratory and animal work done before any testing in people.
- upregulation
- The body producing more of something than it otherwise would.
- clinical trial
- A study that tests something in people under a written plan, with results recorded.
- receptor
- A docking point on a cell. A molecule that fits it can switch a process on or off inside that cell.
- efficacy
- Whether something works under trial conditions, which is not the same as in daily use.
- subcutaneous
- Into the fat layer just under the skin.
Compounding status
Nomination withdrawn- FDA lists it as
- KPV
- What that means
- These substances are not eligible for the policy that applies to substances in category 1. FDA would consider taking action against a compounder for compounding drug products with this bulk drug substance under its general enforcement policies.
Source: Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks, FDA. Content current as of 2026-04-22; read 2026-09-05. This describes what a compounding pharmacy may supply. It is not advice about your own use.
Also given subcutaneous
- LarazotideLarazotide Acetate (AT-1001)Not on either FDA list
- LiraglutideLiraglutide (acylated GLP-1(7-37) analog)Not on either FDA list
- LL-37LL-37 (Cathelicidin Antimicrobial Peptide / hCAP18 C-terminal fragment)Nomination withdrawn
- Melanotan IIMelanotan II (Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2)Nomination withdrawn
- MK-677 (Ibutamoren)Ibutamoren Mesylate (MK-0677, L-163,191)FDA category 2
- MOTS-cMitochondrial Open Reading Frame of the 12S rRNA Type-cNomination withdrawn
Where this came from6 referencesHide
Each one was resolved at PubMed and confirmed to be the work this page cites. Author, title, journal and year come from the PubMed record, not from the page text.
- Antiinflammatory activity of a COOH-terminal fragment of the neuropeptide alpha-MSH
Hiltz ME, Lipton JM. FASEB journal : official publication of the Federation of American Societies for Experimental Biology (1989). PMID 2550304.
- PepT1-mediated tripeptide KPV uptake reduces intestinal inflammation
Dalmasso G, et al.. Gastroenterology (2008). PMID 18061177.
- 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
Land SC. International journal of physiology, pathophysiology and pharmacology (2012). PMID 22837805.
- Dissection of the anti-inflammatory effect of the core and C-terminal (KPV) alpha-melanocyte-stimulating hormone peptides
Getting SJ, Schiöth HB, Perretti M. The Journal of pharmacology and experimental therapeutics (2003). PMID 12750433.
- Orally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis
Xiao B, et al.. Molecular therapy : the journal of the American Society of Gene Therapy (2017). PMID 28143741.
- Critical role of PepT1 in promoting colitis-associated cancer and therapeutic benefits of the anti-inflammatory PepT1-mediated tripeptide KPV in a murine model
Viennois E, et al.. Cellular and molecular gastroenterology and hepatology (2016). PMID 27458604.
About this page
Reviewed 2026-08-11. This page reports what published studies and FDA documents say. It carries no dose, cycle length or stack, and it does not tell you whether a substance is appropriate for you. Side-effect reports circulating on forums are self-reported rather than measured, so they are not republished here.
See the editorial policy for how corrections are handled.