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    DRUG CLASS:

    NRF2 activator

    Related drugs:
    6d
    A Study to Learn About the Safety of BIIB091 and Its Effect on Brain Inflammation When Taken Alone or With Diroximel Fumarate (DRF) in Adults With Relapsing Forms of Multiple Sclerosis (MS) (clinicaltrials.gov)
    P2, N=127, Active, not recruiting, Biogen | Recruiting --> Active, not recruiting | N=275 --> 127
    Enrollment closed • Enrollment change
    7d
    The Role of Iron-Overloaded Macrophages in Mesenchymal Stem Cell Senescence and Anemia in Myelodysplastic Syndromes: Protocol for an In Vitro Study. (PubMed, JMIR Res Protoc)
    This study is expected to elucidate a novel molecular mechanism linking iron overload in macrophages to BMSC dysfunction and anemia in MDS. The findings could identify the Keap1-Nrf2-ARE pathway as a potential therapeutic target for managing MDS-related anemia.
    Preclinical • Journal
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    IL6 (Interleukin 6) • CD68 (CD68 Molecule) • VCAM1 (Vascular Cell Adhesion Molecule 1)
    10d
    A Study to Learn How the Body Processes BIIB141 (Omaveloxolone) When Taken as a Capsule or as a Tablet Dissolved in Liquid, and to Learn About Its Safety in Healthy Adults Ages 18 to 55 (clinicaltrials.gov)
    P1, N=70, Recruiting, Biogen | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Skyclarys (omaveloxolone)
    13d
    A Study to Find Out How BIIB141 (Omaveloxolone) is Processed in the Body and to Learn More About Its Safety in Participants With Friedreich's Ataxia Aged 2 to 15 Years Old (clinicaltrials.gov)
    P1, N=35, Recruiting, Biogen | Trial completion date: Feb 2030 --> Nov 2030
    Trial completion date
    |
    Skyclarys (omaveloxolone)
    20d
    pH-triggered Mn-ZIF8 nanoreactor enhances tumor immunotherapy by amplifying the cGAS-STING pathway through a self-reinforcing gas-metal synergy strategy. (PubMed, J Nanobiotechnology)
    In this study, we propose a Gas-Metal Synergy Strategy, which integrates immune activation and biosafety, by engineering a pH-responsive manganese-based zeolitic imidazolate framework (named MRPH) nanoplatform co-loaded with the nitric oxide (NO) donor RRX-001...Both in vitro and in vivo studies demonstrate that MRPH significantly enhances gas-amplified metalloimmunotherapy. This work pioneers a low-toxicity paradigm that integrates gas therapy and metal-based immunotherapy, offering a transformative approach to solid tumor immunotherapy.
    Journal
    |
    CD8 (cluster of differentiation 8)
    |
    nibrozetone (RRx-001)
    20d
    Effects of the Pharmacological Modulation of NRF2 in Cancer Progression. (PubMed, Medicina (Kaunas))
    In contrast, NRF2 activators, such as bardoxolone methyl (CDDO-Me), sulforaphane, and dimethyl fumarate, exhibit chemopreventive effects by enhancing detoxification and mitigating oxidative DNA damage during early tumorigenesis...Therefore, understanding the temporal and contextual effects of NRF2 signaling is crucial for therapeutic design. The aim of this review is to examine how pharmacological modulation of NRF2 influences the invasive and metastatic dimensions of tumor progression, in addition to discussing its potential integration into TNM-based prognostic and treatment frameworks.
    Review • Journal
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    KEAP1 (Kelch Like ECH Associated Protein 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
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    KEAP1 mutation • NFE2L2 mutation
    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
    |
    KEAP1 (Kelch Like ECH Associated Protein 1)
    |
    KEAP1 mutation
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    Skyclarys (omaveloxolone)
    29d
    A Study to Learn How the Body Processes BIIB141 (Omaveloxolone) When Taken as a Capsule or as a Tablet Dissolved in Liquid, and to Learn About Its Safety in Healthy Adults Ages 18 to 55 (clinicaltrials.gov)
    P1, N=70, Not yet recruiting, Biogen
    New P1 trial
    |
    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
    |
    SLC16A1 (Solute Carrier Family 16 Member 1) • PHGDH (Phosphoglycerate Dehydrogenase)
    |
    Skyclarys (omaveloxolone)
    1m
    E3 Ubiquitin Ligase TRIM47 Promotes Intrahepatic Cholangiocarcinoma Progression by Ubiquitinating Fumarate Hydratase and Modulating Macrophage Polarization. (PubMed, J Biol Chem)
    FH overexpression restored the effects of TRIM47. Collectively, the observations demonstrate that TRIM47 accelerates the progression of ICC by interacting with FH and ubiquitinating FH, indicating that TRIM47/FH axis may be potential target for ICC treatment.
    Journal
    |
    FH (Fumarate Hydratase) • TRIM4 (Tripartite Motif Containing 4) • TRIM47 (Tripartite Motif Containing 47)
    1m
    DARLENE: DIROXIMEL FUMARATE TO REDUCE PERIHAEMATOMAL OEDEMA IN INTRACEREBRAL HAEMORRHAGE: A DOUBLE BLIND RANDOMIZED CLINICAL TRIAL (clinicaltrials.gov)
    P2, N=192, Not yet recruiting, University Hospital, Lille
    New P2 trial
    2ms
    Clinical Study for Dimethyl Fumarate in Preserving Islet β-Cell Function in Type 1 Diabetes Mellitus (clinicaltrials.gov)
    P3, N=90, Not yet recruiting, Nanjing Medical University
    New P3 trial