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Tissue Repair & Anti-Inflammatory

KPV

Anti-inflammatory tripeptide from α-MSH that calms gut and skin inflammation in animals without tanning effects.

RestrictedEvidence level 2 of 5: Animal data, minimal humanAlso: Lys-Pro-Val, α-MSH(11-13), Lysine-Proline-Valine

Overview

KPV is the last three amino acids (lysine-proline-valine) of alpha-melanocyte-stimulating hormone (α-MSH). It keeps much of α-MSH's anti-inflammatory activity but lacks the receptor-binding region responsible for tanning, appetite and sexual effects. In intestinal cells it is taken up by the PepT1 peptide transporter, which is increased in inflamed colon, and then suppresses NF-κB, the master switch for inflammatory cytokines. In mouse models of colitis, oral KPV reduced inflammation and tissue damage, and it has shown benefit in skin inflammation and wound models, along with direct antimicrobial activity. Its safety profile appears benign, but no human efficacy trials have been published, so its use rests on animal data and clinical experience.

Classification
Tripeptide (Lys-Pro-Val), the C-terminal fragment of α-MSH
Route
Oral, subcutaneous or topical
Half-life
Short (minutes systemically); local tissue effects sustained

Mechanism of action

Primary targetIntracellular NF-κB inhibition via PepT1 uptake
  1. Oral, topical or SC dosingOral forms target the gut; topical for skin inflammation.
  2. PepT1 transporter uptakeInflamed intestinal epithelium expresses more PepT1, concentrating KPV where needed.
  3. NF-κB inhibitionBlocks nuclear translocation of the master inflammatory transcription factor.
  4. Cytokine reductionTNF-α, IL-6 and IL-1β production decreases.
  5. Barrier and tissue recoveryReduced inflammation allows mucosal and skin healing.
Downstream effects
  • Reduced gut inflammation
  • Calmer inflamed skin
  • No pigmentation effects

Researched for

  • Inflammatory bowel disease (ulcerative colitis, Crohn's)
  • Eczema and psoriasis
  • Mast cell–related inflammation
  • Wound healing
  • Microbial infections (Candida, S. aureus)

Research notes

  • Dalmasso et al. (2008): oral KPV reduced colitis severity in mice via PepT1-mediated uptake.
  • Laroui et al. (2010): KPV-loaded nanoparticles reduced colitis at very low doses in mice.
  • In vitro studies show antimicrobial activity against S. aureus and Candida albicans.
  • FDA advisory committee recommended inclusion in July 2026 despite FDA staff noting no human efficacy data.

Reported side effects

  • Generally well tolerated in reported use
  • Mild GI upset (oral)
  • Injection-site reactions (SC)
  • Local irritation (topical)

Contraindications & cautions

  • Pregnancy and breastfeeding (no data)
  • Known hypersensitivity
  • Situations requiring an intact inflammatory response (e.g., active serious infection, relative)

Lab monitoring

  • CBC with differential
  • CMP
  • CRP, ESR, hsCRP
  • Fecal calprotectin (IBD)
  • Vitamin D (25-OH)

Dosing and pricing for KPV

Dosing references and compound pricing are available to established patients in the secure portal after a medical evaluation.

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