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DRUG:

fingolimod

i
Other names: FTY 720, TDI-132, FTY-720, FTY720
Company:
Generic mfg.
Drug class:
S1PR modulator
4d
Enrollment change • Trial initiation date
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Briumvi (ublituximab-xiiy) • fingolimod
6d
Polypharmacologic phosphoinositide modulation by FTY720 triggers endomembrane trafficking collapse and metabolic starvation in cancer cells. (PubMed, Biochem Biophys Res Commun)
Building on our work with the structurally related compound KRP203, we show that high-dose FTY720 produces isozyme-divergent modulation across phosphoinositide kinases and biases PIKFYVE activity toward phosphatidylinositol, a pattern we term ASURA (Asymmetric Simultaneous Uncoupling of Related Activities). Patient-derived glioblastoma (GBM) neurospheres were sensitive to FTY720, and co-treatment with a PI3Kα-selective inhibitor augmented growth suppression in U87MG cells. Together, these data support a model in which ASURA-dose FTY720 disrupts phosphoinositide-regulated trafficking and nutrient access, imposing intracellular nutrient stress that culminates in tumor-cell death.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
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fingolimod • mocravimod (KRP-203)
6d
New P2/3 trial
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Briumvi (ublituximab-xiiy) • fingolimod
1m
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
2ms
NEOS: Efficacy and Safety of Ofatumumab and Siponimod Compared to Fingolimod in Pediatric Patients With Multiple Sclerosis (clinicaltrials.gov)
P3, N=129, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Nov 2031 --> Mar 2031
Trial completion date • Head-to-Head
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fingolimod
2ms
NEOS: Efficacy and Safety of Ofatumumab and Siponimod Compared to Fingolimod in Pediatric Patients With Multiple Sclerosis (clinicaltrials.gov)
P3, N=129, Active, not recruiting, Novartis Pharmaceuticals | Trial primary completion date: Mar 2027 --> Apr 2026
Trial primary completion date • Head-to-Head
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fingolimod
2ms
New P2/3 trial
|
Briumvi (ublituximab-xiiy) • fingolimod
2ms
Study to Assess Effects of Ublituximab in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (clinicaltrials.gov)
P2/3, N=240, Not yet recruiting, TG Therapeutics, Inc. | Initiation date: Dec 2025 --> Mar 2026
Trial initiation date
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Briumvi (ublituximab-xiiy) • fingolimod
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)
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fingolimod