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DRUG:

Tavalisse (fostamatinib)

i
Other names: R935788, R788, R788 sodium, R-985788, FosD, R406, R940406, R 985788, R-406/788, R-788, R-935/788, IMG-016, IMG016, IMG 016, R985788, R 406/788, R406/788, R 935/788, R935/788, R 935788, R-935788, R-940406, R 940406
Company:
Grifols, JW Pharma, Kissei, Knight Therap, Mitsubishi Tanabe, Rigel
Drug class:
SYK inhibitor
16d
Inflammatory Signal Inhibitors for COVID-19 (MATIS) (clinicaltrials.gov)
P1/2, N=185, Completed, Imperial College London | Recruiting --> Completed | N=456 --> 185
Trial completion • Enrollment change
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CRP (C-reactive protein)
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Jakafi (ruxolitinib) • Tavalisse (fostamatinib)
22d
Network Controllability Reveals Key Mitigation Points for Tumor-Promoting Signaling in Tumor-Educated Platelets. (PubMed, Int J Mol Sci)
A low-dose combination therapy of fostamatinib, Aducanumab, and acetylsalicylic acid (aspirin) may control TEP effects. In conclusion, our preclinical in silico approach revealed FDA-approved drugs that allow therapeutic targeting of metastasis-promoting TEPs and target NSCLC at the same time.
Journal
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SYK (Spleen tyrosine kinase) • FCGR2A (Fc fragment of IgG receptor IIa) • ITGA2B (Integrin Subunit Alpha 2b)
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Tavalisse (fostamatinib) • aspirin
24d
Extension Study (Extended Access) of Syk-inhibition Using Fostamatinib to Treat Posttransplant Immune-mediated Cytopenias (clinicaltrials.gov)
P2, N=0, Withdrawn, National Heart, Lung, and Blood Institute (NHLBI) | N=20 --> 0 | Trial completion date: Dec 2028 --> Nov 2025 | Enrolling by invitation --> Withdrawn | Trial primary completion date: Dec 2028 --> Nov 2025
Enrollment change • Trial completion date • Trial withdrawal • Trial primary completion date
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Tavalisse (fostamatinib)
1m
Using Fostamatinib to Treat Post-Hematopoietic Stem Cell Transplant Immune-mediated Cytopenias (clinicaltrials.gov)
P2, N=1, Completed, National Heart, Lung, and Blood Institute (NHLBI) | Recruiting --> Completed | N=20 --> 1 | Trial completion date: Apr 2026 --> Oct 2025 | Trial primary completion date: Apr 2026 --> Oct 2025
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
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Tavalisse (fostamatinib)
3ms
Study to Evaluate the Safety and Tolerability of Escalating Doses of Fostamatinib in Subjects With Stable Sickle Cell Disease (clinicaltrials.gov)
P1, N=25, Recruiting, National Heart, Lung, and Blood Institute (NHLBI) | Trial primary completion date: Aug 2025 --> May 2026
Trial primary completion date
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Tavalisse (fostamatinib)
3ms
NEK9-mediated Wnt signalling repressor TLE3 rewires Docetaxel resistance in cancer cells by inducing pyroptosis. (PubMed, Br J Cancer)
Our study demonstrated that NEK9 plays an important role in Docetaxel resistance. The novel combination of NEK9 inhibitor Fostamatinib and Docetaxel needs further clinical investigation in advanced OSCC.
Journal
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TLE3 (TLE Family Member 3, Transcriptional Corepressor)
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docetaxel • Tavalisse (fostamatinib)
5ms
Integrative machine learning and structure-based drug repurposing for identifying potent inhibitors of human SYK activity against cancer. (PubMed, Life Sci)
Despite the investigation of inhibitors of SYK including fostamatinib, entospletinib, cerdulatinib, and TAK-659 for cancer therapy, their lack of specificity and potential off-target effects remain significant concerns...Rifabutin, darunavir, and sildenafil were found as promising SYK inhibitors, showing strong interactions and stable conformations...Our findings underscore the value of computational methods in drug discovery and advocate for further experimental validation of these compounds as SYK-targeted therapies. This study aims to advance the development of more effective and safer treatments for cancers associated with SYK overexpression.
Journal
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SYK (Spleen tyrosine kinase)
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entospletinib (GS-9973) • mivavotinib (CB-659) • Tavalisse (fostamatinib) • sildenafil
6ms
FOSTA-ARDS: Fostamatinib for Treating Acute Respiratory Distress Syndrome (ARDS) in Hospitalized Adults (clinicaltrials.gov)
P2, N=40, Not yet recruiting, Inova Health Care Services | Initiation date: May 2025 --> Jul 2025
Trial initiation date
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Tavalisse (fostamatinib)
6ms
Drug repurposing of fostamatinib against cancer via potential cytotoxicity and immune checkpoint regulation. (PubMed, Front Immunol)
Moreover, fostamatinib downregulated the expression of immune checkpoints such as PD-L1 and CD47. Overall, this study provided a conceptual foundation for evaluating the advantages of drug repurposing in AML drug development.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • FLT3 (Fms-related tyrosine kinase 3) • SYK (Spleen tyrosine kinase)
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Tavalisse (fostamatinib)
7ms
125I inhibits the progression of cervical cancer by upregulating the HSF1/PU.1/SYK signaling pathway and consequently enhancing the apoptotic response mediated by ROS/USP7/P53. (PubMed, Sci Rep)
However, specific knockdown of HSF1 and the administration of the SYK inhibitor R406 can reverse the potentiating effect of 125I radiotherapy on the ROS/USP7/P53 pathway, consequently promoting the progression of cervical cancer; specific overexpression of PU.1 can abrogate the inhibitory impact of HSF1 knockdown on the ROS/USP7/P53 pathway, thereby suppressing the progression of cervical cancer. 125I inhibits the progression of cervical cancer by upregulating the HSF1/PU.1/SYK signaling pathway and consequently enhancing the apoptotic response mediated by ROS/USP7/P53.
Journal
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SYK (Spleen tyrosine kinase) • CLEC7A (C-Type Lectin Domain Containing 7A) • HSF1 (Heat Shock Transcription Factor 1) • USP7 (Ubiquitin Specific Peptidase 7)
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Tavalisse (fostamatinib)
7ms
Interpretable Machine Learning reveals the Role of PANoptosis in the Diagnosis and Subtyping of NAFLD. (PubMed, Immunobiology)
Molecular docking studies identified fostamatinib and minocycline as potential therapeutic candidates, while pan-cancer analysis revealed that TNFRSF1A overexpression is associated with poor prognosis across multiple cancer types. This study enhances the understanding of PANoptosis as a crucial diagnostic and therapeutic target in NAFLD, providing novel insights into immune-mediated pathogenesis and paving the way for treatment strategies.
Journal
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TNFAIP3 (TNF Alpha Induced Protein 3) • TNFRSF1A (TNF Receptor Superfamily Member 1A) • CASP6 (Caspase 6, apoptosis-related cysteine peptidase)
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Tavalisse (fostamatinib) • minocycline
7ms
Real World Evaluation of the Activity and Safety of Fostamatinib in Consecutive Adult Patients With ITP (clinicaltrials.gov)
P=N/A, N=95, Completed, Gruppo Italiano Malattie EMatologiche dell'Adulto | Not yet recruiting --> Completed | N=47 --> 95 | Trial completion date: Dec 2023 --> May 2024 | Trial primary completion date: Dec 2023 --> May 2024
Trial completion • Enrollment change • Trial completion date • Trial primary completion date • HEOR • Real-world evidence
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Tavalisse (fostamatinib)