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DRUG CLASS:

S1PR modulator

3d
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
6d
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)
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Avastin (bevacizumab) • fingolimod
17d
Enrollment open
26d
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
1m
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
1m
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)
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fingolimod
2ms
Enrollment open
2ms
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
2ms
New P1 trial
3ms
An epigenetic switch in vascular phenotype augments anti-tumor immunity. (PubMed, bioRxiv)
Depleting CD4+ T-cells, or blocking lymphocyte egress from the lymph nodes with FTY720, rescues tumor growth in mice with conditional deletion of Dnmt1 in ECs (Dnmt1iECKO) and dramatically shortens overall survival, whereas NK cells are dispensable...Finally, immune checkpoint blockade (ICB) administered to Dnmt1iECKO mice with experimental melanoma lung metastasis reduces tumor burden, with some mice showing tumor eradication. Our findings identify endothelial Dnmt1 as a key regulator of vascular-mediated anti-tumor immunity, providing a rationale for integrating epigenetic modulation of the vasculature with cancer immunotherapy regimens.
Journal • IO biomarker
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TNFA (Tumor Necrosis Factor-Alpha) • DNMT1 (DNA methyltransferase 1) • CD40 (CD40 Molecule) • TNFSF4 (TNF Superfamily Member 4) • VCAM1 (Vascular Cell Adhesion Molecule 1)
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fingolimod