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    DRUG CLASS:

    S1PR modulator

    Related drugs:
    4d
    Loss of oligodendrocyte transcription factor 2 protein expression in metabolically stressed oligodendrocytes. (PubMed, Acta Neuropathol)
    Pharmacological intervention with the sphingosine-1-phosphate receptor modulator siponimod during cuprizone intoxication attenuated OLIG2 protein loss, indicating that this stress-induced state is pharmacologically modifiable...Thus, OLIG2 protein loss may serve as an early indicator of oligodendrocyte stress and a possible therapeutic target for preserving myelin integrity in demyelinating disorders. These findings have additional methodological implications as stressed oligodendrocytes may evade detection using OLIG2-based lineage markers.
    Journal
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    ATF3 (Activating Transcription Factor 3) • OLIG2 (Oligodendrocyte Transcription Factor 2)
    25d
    SIPO1-AD: Repurposing Siponimod for Alzheimer's Disease (clinicaltrials.gov)
    P2, N=105, Recruiting, St. Joseph's Hospital and Medical Center, Phoenix | Not yet recruiting --> Recruiting
    Enrollment open
    28d
    Bevacizumab and Fingolimod Combination Therapy Induce Cytotoxicity and Apoptosis in Ovcar-3 Cells. (PubMed, Anticancer Agents Med Chem)
    The combination of Bevacizumab and Fingolimod presents a promising treatment strategy for ovarian cancer.
    Journal
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    CASP3 (Caspase 3) • CASP7 (Caspase 7) • ANXA5 (Annexin A5)
    |
    Avastin (bevacizumab) • fingolimod
    1m
    A Research Trial to Assess if Cenerimod is Efficacious and Safe to Treat Active Lupus Nephritis on Top of Regular Treatment (clinicaltrials.gov)
    P3, N=300, Recruiting, Viatris Innovation GmbH | Not yet recruiting --> Recruiting
    Enrollment open
    1m
    ID-064-108: A trial to evaluate the absolute bioavailability of cenerimod in healthy male participants (2025-522320-27-00)
    P1, N=6, Recruiting, Viatris Innovation GmbH
    New P1 trial
    2ms
    OPUS-2: A Research Study to Evaluate the Efficacy and Safety of Cenerimod in Subjects Suffering From Systemic Lupus Erythematosus (clinicaltrials.gov)
    P3, N=451, Active, not recruiting, Viatris Innovation GmbH | Recruiting --> Active, not recruiting
    Enrollment closed
    2ms
    SPHK1 deficiency promotes intestinal homeostasis by ameliorating ER stress-induced gastrointestinal injury during murine graft-versus-host disease. (PubMed, Sci China Life Sci)
    FTY720, an S1P receptor antagonist, significantly inhibits ER stress-induced IEC injury. Our findings highlight the pathogenic role of host SPHK1 in gastrointestinal injury during aGVHD and suggest that targeting SPHK1 could be a therapeutic strategy for managing this condition.
    Preclinical • Journal
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    SPHK1 (Sphingosine Kinase 1)
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    fingolimod
    2ms
    In-silico characterization of deleterious non-synonymous SNPs in the human S1PR1 gene reveals structural instability and altered ligand affinity. (PubMed, PLoS One)
    Molecular docking and dynamics simulations showed that R120P and F125S weaken binding affinity for natural agonist sphingosine-1-phosphate (S1P) and FTY720P, while antagonist W146 retained strong binding...Collectively, these findings identified high-risk nsSNPs in S1PR1 gene with potential structural and functional implications, particularly in diseases involving impaired receptor signaling. These findings enhanced our understanding of how specific nsSNPs can influence disease susceptibility, drug response, and receptor function, paving the way for precision medicine approaches in treating autoimmune and inflammatory disorders.
    Journal
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    S1PR1 (Sphingosine-1-Phosphate Receptor 1)
    |
    fingolimod
    2ms
    A Study to Evaluate the Safety,Tolerability,Pharmacokinetics and Pharmacodynamics of Cenerimod in Adult Chinese Participants With Moderate-to-severe Systemic Lupus Erythematosus (SLE) (clinicaltrials.gov)
    P2, N=15, Enrolling by invitation, Viatris Pharmaceuticals Co., Ltd. | Not yet recruiting --> Enrolling by invitation
    Enrollment open
    3ms
    A Trial to Evaluate the Absolute Bioavailability of Cenerimod in Healthy Male Participants (clinicaltrials.gov)
    P1, N=6, Active, not recruiting, Viatris Innovation GmbH | Not yet recruiting --> Active, not recruiting
    Enrollment closed
    3ms
    A Trial to Evaluate the Absolute Bioavailability of Cenerimod in Healthy Male Participants (clinicaltrials.gov)
    P1, N=6, Not yet recruiting, Viatris Innovation GmbH
    New P1 trial