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    DRUG CLASS:

    NRF2 activator

    Related drugs:
    4d
    F-53B exacerbates doxorubicin-induced cardiotoxicity by impairing NRF2-dependent ferroptosis defense. (PubMed, Chem Biol Interact)
    Pharmacological activation of NRF2 by dimethyl fumarate (DMF) effectively counteracted the F-53B-induced suppression of GPX4 and FTH1, thereby alleviating ferroptosis and the ensuing cardiotoxicity. Collectively, our findings reveal the synergistic impact of F-53B and DOX on cardiotoxicity and elucidate the underlying mechanism involving the NRF2-mediated anti-ferroptosis pathway.
    Journal
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    GPX4 (Glutathione Peroxidase 4)
    |
    doxorubicin hydrochloride
    17d
    A Study to Learn More About The Safety of Diroximel Fumarate (VUMERITY®) in Participants Who Took it During Pregnancy And About the Health of Their Babies (clinicaltrials.gov)
    P=N/A, N=1178, Active, not recruiting, Biogen | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    fingolimod • Lemtrada (alemtuzumab) • Ocrevus (ocrelizumab) • Tysabri (natalizumab)
    22d
    A Study to Evaluate the Safety, Tolerability, and Efficacy of TML-6 in Participants With Early Alzheimer's Disease (clinicaltrials.gov)
    P2, N=210, Not yet recruiting, Merry Life Biomedical Co., Ltd.
    New P2 trial
    27d
    Esculeoside A attenuates aortic remodeling and early atherosclerosis-like changes, with protective effects strongly associated with Nrf2 activation in high-cholesterol-fed rats. (PubMed, Sci Rep)
    Notably, co-administration of brusatol abolished these effects, findings that are consistent with and strongly associated with Nrf2 activation; however, this mechanistic inference is based on pharmacologic inhibition. Collectively, ESA confers robust vascular protection against HCD-induced aortic remodeling and early atherosclerosis-like changes, with these effects being strongly associated with Nrf2 activation.
    Preclinical • Journal • IO biomarker
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    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CAT (Catalase)
    30d
    NRF2 activation by myeloid cell-derived oxidative stress induces SNAI-driven features of EMT in breast cancer. (PubMed, Proc Natl Acad Sci U S A)
    Additionally, high expression of NOX2 subunit genes and SNAI1 associated with reduced metastasis-free survival. These findings imply that myeloid cell-derived ROS initiate partial EMT in breast cancer cells to promote dissemination and that strategies to target myeloid cell-derived ROS may be explored to limit metastasis.
    Journal
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    SNAI1 (Snail Family Transcriptional Repressor 1)
    1m
    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, Completed, Biogen | Recruiting --> Completed
    Trial completion
    |
    Skyclarys (omaveloxolone)
    1m
    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=33, Active, not recruiting, Biogen | Trial primary completion date: Feb 2030 --> Sep 2025 | Recruiting --> Active, not recruiting
    Enrollment closed • Trial primary completion date
    |
    Skyclarys (omaveloxolone)
    2ms
    Efficacy of Omaveloxolone Treatment for Dysphagia in French Patients With Friedreich's Ataxia (clinicaltrials.gov)
    P=N/A, N=40, Recruiting, Centre Hospitalier Universitaire de Nice | Not yet recruiting --> Recruiting | Trial completion date: Oct 2025 --> Jun 2026 | Trial primary completion date: Sep 2025 --> Jun 2026
    Enrollment open • Trial completion date • Trial primary completion date
    |
    Skyclarys (omaveloxolone)
    2ms
    Lycorine suppresses DPP3-mediated Nrf2 signaling, thereby reducing SLC7A11 levels to trigger ferroptosis in colorectal cancer cells. (PubMed, Phytomedicine)
    Lycorine can directly bind to and inhibit DPP3, thereby blocking the Nrf2 signaling pathway and downregulating SLC7A11. This disruption of GSH metabolism leads to the accumulation of ROS and iron overload, ultimately inducing ferroptosis in CRC cells.
    Journal
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    SLC7A11 (Solute Carrier Family 7 Member 11) • DPP3 (Dipeptidyl Peptidase 3)
    2ms
    RTA‑408 induces p38‑dependent apoptosis and suppresses cell viability in hepatocellular carcinoma cells. (PubMed, Hepat Oncol)
    Inhibition of p38 partially restored cell viability and reduced apoptosis. RTA-408 suppresses HCC cell survival through a p38-dependent stress response associated with NRF2 activation and LC3B/p62 accumulation.
    Journal
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    NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • CASP3 (Caspase 3) • ANXA5 (Annexin A5)
    |
    Skyclarys (omaveloxolone)
    2ms
    A Study to Evaluate the Effect of Food on the Bioavailability of AJ201, and Safety, Tolerability, and Pharmacokinetics of AJ201 in Japanese and White Healthy Male Participants (clinicaltrials.gov)
    P1, N=26, Recruiting, AnnJi Pharmaceutical Co., Ltd.
    New P1 trial
    2ms
    DARLENE: DIROXIMEL FUMARATE TO REDUCE PERIHAEMATOMAL OEDEMA IN INTRACEREBRAL HAEMORRHAGE: DOUBLE BLIND RANDOMIZED CLINICAL TRIAL (clinicaltrials.gov)
    P2, N=192, Recruiting, University Hospital, Lille | Not yet recruiting --> Recruiting
    Enrollment open