Educational reference only. Not medical advice. Consult a healthcare provider before starting any protocol.
KPV
Lysine-Proline-Valine (α-MSH C-terminal tripeptide)
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.
Community-reported ranges
Preclinical literature only. Community dosing ranges are anecdotal with no clinical validation. Not dosing guidance.
Reported dose range
200–1500 mcg
Estimated half-life
~1-2 hours (estimated)
Source: General peptide pharmacology principles; no dedicated human PK studies exist
Reported cycle length
2–4 weeks on
2-4 weeks off
Route
subcutaneous, oral, topical
Common vial sizes
5mg, 10mg
Reported timing
AM or split AM/PM
Reported frequency
1x daily
Frequently discussed alongside
Based on community forum discussions. Not a recommendation to combine compounds.
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).
Reported side effects
From community self-reports. Not from controlled studies.
Preclinical models describe KPV as having no notable side effects with no cytotoxicity detected across multiple cell lines. Community reports mention mild injection site irritation, occasional GI upset at higher oral doses, and transient headache or fatigue, though none is consistently reproduced. FDA has flagged the complete lack of human safety data as a concern. Long-term safety is entirely unknown.
Regulatory status
FDA (United States)
Not approved. No clinical trials. FDA Category 2 bulk drug substance since September 2023 — compounding prohibited. HHS Secretary announced potential reclassification to Category 1 on Feb 27, 2026, but not formally enacted as of March 16, 2026.
Health Canada
Not authorized as a therapeutic product. No DIN assigned. Not submitted.
WADA (Competitive Athletes)
Not specifically named on the Prohibited List. As an unapproved substance, it potentially falls under S0 (Non-approved Substances). Mechanistically distinct from prohibited melanocortin agonists — its studied effect is PepT1-mediated, not MCR-mediated. Status is ambiguous; athletes should exercise caution.
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