Bardoxolone methyl
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| ECHA InfoCard | 100.132.153 |
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| Formula | C32H43NO4 |
| Molar mass | 505.69 g/mol |
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Bardoxolone methyl (also known as “RTA 402”, “CDDO-methyl ester”, and CDDO-Me) is an experimental and orally-bioavailable semi-synthetic triterpenoid, based on the scaffold of the natural product oleanolic acid. Pre-clinical studies indicate that the compound acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. A phase 3 clinical trial evaluating bardoxolone methyl for the treatment of chronic kidney disease (CKD) was terminated in October 2012 after patients treated with the drug were found to have experienced a higher rate of heart-related adverse events, including heart failure, hospitalizations, and deaths.
Investigations of bardoxolone methyl have been conducted by Reata Pharmaceuticals in a partnership with Abbvie and Kyowa Hakko Kirin.
A Phase 1 clinical trial, sponsored by Reata, was conducted to determine the safety profile of and appropriate dosing for subsequent phase II studies, as well as to evaluate antitumor activity in patients with advanced solid tumor or lymphoid malignancy. Grade 3 reversible liver transaminase elevations were reported. The maximum tolerated dose was 900 mg/day. NQO1 mRNA levels, indicative of Nrf2 pathway activation, were increased in peripheral blood mononuclear cells (PBMCs), and tumor biopsies showed decreased levels of NF-κB and cyclin D1. An improvement in estimated glomerular filtration rate (eGFR) in patients treated with bardoxolone methyl was noted, and based on this finding it was suggested by the authors that the drug might be beneficial for patients with CKD.
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