Drug intelligence / Profile preview

bardoxolone methyl

Development stage
Phase 3
Lead developer
Biogen
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Bardoxolone methyl is an orally bioavailable, semi-synthetic triterpenoid derived from oleanolic acid. It acts primarily as an activator of the Nrf2 pathway and inhibitor of the NF-kappaB pathway. These mechanisms confer anti-inflammatory and cytoprotective effects by upregulating antioxidant response elements and suppressing pro-inflammatory gene expression. Bardoxolone methyl has been investigated for chronic kidney diseases (including Alport syndrome, diabetic kidney disease, autosomal dominant polycystic kidney disease), pulmonary arterial hypertension, and cancer. Despite initial promise in improving estimated glomerular filtration rate (eGFR) in chronic kidney disease patients, several phase 3 trials were terminated due to lack of efficacy or safety concerns related to cardiovascular events[2][7][10]. The drug was developed by Reata Pharmaceuticals with Kyowa Kirin as a strategic collaborator for some indications.

Brand names
RTA 402RTA402RTA-402
Other names
methyl bardoxolonatebardoxolone methyl estermethyl 2-cyano-3,12-dioxooleana-1,9-dien-28-oate
02

Targets

KEAP1 (Kelch-like ECH-associated protein 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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