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DRUG:

Skyclarys (omaveloxolone)

i
Other names: RTA 408, RTA-408, ABT-RTA-408, RTA408, BIIB141
Associations
Company:
Biogen
Drug class:
NRF2 activator
Associations
13d
Trial completion date
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Skyclarys (omaveloxolone)
21d
Synthetic Oleanane Triterpenoids Reduce Tumor Growth and Promote an Anti-Tumor Immune Response Independent of Cancer KEAP1 Mutational Status. (PubMed, Antioxidants (Basel))
Similarly, subcutaneous KEAP1 KO tumors were larger and more immune-suppressed compared to WT tumors. Both CDDO-Me and omaveloxolone reduced the tumor burden and improved immune cell phenotypes within the TIME independent of KEAP1 mutational status.
Journal
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KEAP1 (Kelch Like ECH Associated Protein 1)
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KEAP1 mutation
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Skyclarys (omaveloxolone)
1m
The role of glutamine/Nrf2-enhanced PHGDH in Cadmium-induced lactate utilization. (PubMed, Free Radic Biol Med)
Moreover, inhibition of Nrf2 with ML385 attenuated Cd-induced glutamine metabolism, PHGDH, MCT1, lactate production, and cell migration, while activation of Nrf2 with RTA-408 had the opposite effect...Collectively, these findings suggest that PHGDH plays a crucial role in Cd-induced lactate utilization, and the mechanism underlies the interaction between glutamine and Nrf2. This study provides insights into the mechanism of Cd-related tumorigenesis and toxicity.
Journal
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SLC16A1 (Solute Carrier Family 16 Member 1) • PHGDH (Phosphoglycerate Dehydrogenase)
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Skyclarys (omaveloxolone)
2ms
Attenuation of cerebral ischemia-reperfusion induced neurotoxicity by telmisartan, ertugliflozin, and omaveloxolone through Nrf2/HO-1 pathway modulation: In vivo and in silico insights. (PubMed, Toxicol Rep)
In silico analysis revealed strong binding through highly negative docking scores of telmisartan and ertugliflozin to Nrf2 negative regulators Keap1 and GSK-3β, supported by stable molecular dynamics simulations, suggesting direct inhibition. In conclusion, omaveloxolone, telmisartan, and ertugliflozin alleviate ischemia-reperfusion induced neurotoxicity via potential Nrf2-mediated antioxidant and anti-inflammatory mechanisms, highlighting their potential preventive role in conditions predisposing to stroke.
Preclinical • Journal
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KEAP1 (Kelch Like ECH Associated Protein 1) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • MMP9 (Matrix metallopeptidase 9)
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Skyclarys (omaveloxolone)
2ms
RTA-408 Enhances Radiosensitivity and Inhibited Tumor Progression via JNK Pathway in Glioblastoma. (PubMed, Kaohsiung J Med Sci)
RTA-408 exerts antitumour and radiosensitizing effects via activation of the JNK pathway and inhibits GBM progression. These findings highlight its potential as a novel therapeutic strategy for the treatment of GBM.
Journal
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CCND1 (Cyclin D1)
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Skyclarys (omaveloxolone)
3ms
Trial completion
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Skyclarys (omaveloxolone) • omeprazole
4ms
Trial completion
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Skyclarys (omaveloxolone)
4ms
Enrollment open
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Skyclarys (omaveloxolone) • omeprazole
5ms
KIAA1429 Silencing ameliorates osteosarcoma progression through promoting ferroptosis via Nrf2/NQO1 axis. (PubMed, Inflamm Res)
KIAA1429 silencing facilitates ferroptosis, thereby delaying OS progression, potentially through modulation of the Nrf2/NQO1 signaling pathway.
Journal
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NQO1 (NAD(P)H dehydrogenase, quinone 1) • VIRMA (Vir Like M6A Methyltransferase Associated)
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erastin • Skyclarys (omaveloxolone)