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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
6d
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)
2ms
Trial completion
|
Skyclarys (omaveloxolone)
3ms
Enrollment open
|
Skyclarys (omaveloxolone)
4ms
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)
4ms
Enrollment open
|
Skyclarys (omaveloxolone)
5ms
Synthetic oleanolic acid derivative, RTA-408, overcome in TMZ-resistant glioblastoma cells by inducing apoptosis and G1 cell cycle arrest. (PubMed, Med Oncol)
Western blot analysis revealed that RTA-408 modulated apoptosis-related protein expression and inhibited reactive oxygen species production, thereby reducing oxidative stress in TMZ-resistant glioblastoma cells. These findings indicate that RTA-408 is not only a promising alternative for TMZ-sensitive glioblastoma but also a first-line treatment option for TMZ-resistant glioblastoma.
Journal
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KEAP1 (Kelch Like ECH Associated Protein 1) • CASP3 (Caspase 3)
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Skyclarys (omaveloxolone)
5ms
The Central Role of NRF2 in Cancer Metabolism and Redox Signaling: Novel Insights into Crosstalk with ER Stress and Therapeutic Modulation. (PubMed, Cell Biochem Biophys)
Additionally, we explore the complementary role of NRF1, an ER-resident transcription factor that cooperates with NRF2 to maintain proteostasis and mediate stress resilience. Finally, we examine the therapeutic landscape of NRF2-targeted agents including ML385, PRL295, Omaveloxolone, and DHTI, highlighting their potential for therapeutic use tailored to tumor stage and cellular context.
Review • Journal
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NRF1 (Nuclear Respiratory Factor 1)
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Skyclarys (omaveloxolone)
5ms
RTA-408 overcomes cisplatin-resistant lung cancer by inhibiting WWP1-mediated NCOA4 ubiquitination to induce ferritinophagy and ferroptosis. (PubMed, Free Radic Biol Med)
We selected A549/DDP cells as a research model and demonstrated through a series of experimental manipulations that RTA-408 inhibited the growth of A549/DDP cells and inhibited the ubiquitinated degradation of nuclear receptor coactivator 4 through down-regulation of WW structural domain-containing E3 ubiquitin-protein ligase 1 (WWP1), which further induced the development of ferritinophagy and ferroptosis. We report for the first time that RTA-408 overcomes cisplatin-resistant lung cancer by targeting WWP1-mediated ferritinophagy and ferroptosis.
Journal
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NCOA4 (Nuclear Receptor Coactivator 4) • UBR5 (Ubiquitin Protein Ligase E3 Component N-Recognin 5)
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cisplatin • Skyclarys (omaveloxolone)
6ms
Enrollment open
|
Skyclarys (omaveloxolone)