KPV is a naturally occurring tripeptide (Lys-Pro-Val, MW ~342.4 g/mol) derived from the C-terminal region (positions 11–13) of alpha-melanocyte-stimulating hormone (α-MSH). It retains potent anti-inflammatory and antimicrobial properties of the full-length hormone without activating melanocortin receptors responsible for skin pigmentation or sexual arousal. KPV suppresses NF-κB activation and is transported into intestinal epithelial cells via the PepT1 transporter, which is upregulated during gut inflammation — creating a self-targeting mechanism. Its small size enables oral bioavailability, which is unusual for peptides. It was among the 12 peptides removed from FDA Category 2 on April 15, 2026.
Category: Anti-Inflammatory / Immune. Evidence rating: D (animal/preclinical only).
Clinical status: Preclinical. No formal clinical trials completed. Used in compounding pharmacy protocols. Removed from FDA Category 2 on April 15, 2026.
KPV exerts anti-inflammatory effects through a mechanism distinct from the parent α-MSH hormone. Rather than acting through melanocortin receptors (which would trigger pigmentation), KPV is transported into cells via PepT1, a di/tripeptide transporter expressed on intestinal epithelial cells and…
Research base: 0 registered clinical trials and 4 indexed publications reference KPV.
Safety considerations: No significant adverse effects reported in preclinical studies; Does not cause skin darkening (unlike Melanotan peptides); No formal human safety trials have been conducted.
Reviewed by the PeptideAtlas Editorial Team. Last reviewed: 2026-08-12.
KPV is the C-terminal fragment of α-MSH and does NOT cause skin darkening. Melanotan I and II are full melanocortin receptor agonists that cause pigmentation. KPV works through the PepT1 transporter, not melanocortin receptors, so it provides anti-inflammatory benefits without tanning effects.
Yes. Oral KPV is commonly used for gut inflammation because the PepT1 transporter in intestinal cells actively imports it. PepT1 is upregulated during gut inflammation, creating a self-targeting mechanism. Typical oral doses are 200-500 mcg, 1-2 times daily.
No. KPV has no FDA approval and has not completed formal clinical trials in humans. It was removed from FDA Category 2 on April 15, 2026, and PCAC review is scheduled for July 2026.