Drug intelligence / Profile preview

kavain

Development stage
Preclinical
Lead developer
University of California, Irvine
Modality
Small Molecules
Administration
Oral
01

Overview

Kavain (also spelled kawain) is a major kavalactone found in the roots of the kava plant (*Piper methysticum*). It has been investigated for its potential chemopreventive and therapeutic effects in various cancers, particularly urinary bladder cancer. Mechanistically, kavain acts as an epigenetic modulator by inhibiting lysine-specific demethylase 1 (LSD1/KDM1A), which leads to increased histone methylation (specifically H3K4 me1/me2 and H3K9 me2) in malignant cells. In preclinical models, kavain has demonstrated the ability to selectively inhibit the growth of bladder cancer cells and slow the progression of chemically induced bladder carcinogenesis. Beyond its potential oncology applications, kavalactones are traditionally known for their anxiolytic and sedative properties, which are mediated through the modulation of GABAergic signaling and voltage-gated sodium and calcium channels.

Other names
kawain(R)-kavain5,6-dihydro-4-methoxy-6-(2-phenylethenyl)-2H-pyran-2-one
02

Targets

GABRR (GABA-A receptor subunit rho)KDM1A (LSD1)

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