Bardoxolone is a synthetic oleanane triterpenoid that exerts multifunctional activities in the control of cellular growth and differentiation. Bardoxolone is capable of activating the transcription fa
ctor peroxisome proliferator activator receptor-γ (PPARγ), its apoptotic effects in malignant cells have been shown to occur independently of PPARγ. Bardoxolone was developed as an potential drug for
the improvement of hyperglycemia, proteinuria, glomerulus structure, serum creatine, which may in turn be beneficial to treat diabetic kidney diseases, cancer and thromboembolic events.
ChEBI: Bardoxolone is a member of cyclohexenones.
bardoxolone methyl, previously known as rta 402, is the lead molecule in reata's portfolio of antioxidant inflammation modulators (aims). the aims are potent inducers of the transcription factor nrf2, an important biological target that controls the production of many of the body's antioxidant and detoxification enzymes. because oxidative stress and inflammation occur throughout the course of chronic kidney disease (ckd) and are known to contribute to loss of kidney function, agents that activate the nrf2 pathway in patients with ckd may provide a novel method for preserving or improving kidney function. bardoxolone methyl is currently being investigated as a potential oral once-a-day treatment for ckd.
Bardoxolone methyl(5, 10 mg/kg) decreased the percentage of caspase-3 immunopositive cells in a dose-dependent manner in rat kidney [3].
Bardoxolone methyl (0-10 mg/kg, i.p., a single dose) results in analgesia but not sedation in rats[4].
Bardoxolone methyl [10 mg/kg, twice-daily on day 21 after the first PAC (HY-B0015) injection] decreases PAC-induced levels of pNFκB and MCP-1 by increasing pNRf2 and HO-1 in rat DRG[4].
