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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
1d
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 | Trial completion date: Oct 2026 --> Oct 2027 | Trial primary completion date: May 2026 --> May 2027
Trial completion date • Trial primary completion date
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Tavalisse (fostamatinib)
25d
MiR-31 suppresses lung adenocarcinoma cell proliferation through CDK1 and E2F2-mediated cell cycle arrest. (PubMed, Discov Oncol)
Collectively, our study establishes miR-31 as a novel biomarker for LUAD proliferative potential and implicates the miR-31/CDK1-E2F2 network as a promising target for disrupting LUAD progression. These findings establish a miRNA-centric precision therapeutic paradigm for effectively suppressing oncogenic proliferation in LUAD.
Journal
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EGF (Epidermal growth factor) • CDK1 (Cyclin-dependent kinase 1) • MIR31 (MicroRNA 31) • E2F2 (E2F Transcription Factor 2)
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Tavalisse (fostamatinib)
27d
The small-molecule Syk inhibitor R788 inhibits hematopoiesis and worsens anemia in sickle cell disease mice. (PubMed, Blood Vessel Thromb Hemost)
Severe anemia and neutropenia induced by R788 in the sickle mouse model suggests that concomitant use of Syk inhibitors with hydroxyurea in patients with SCD should be approached cautiously. Further research is required to clarify the benefits and risks of selective Syk inhibition in SCD and other hemolytic conditions exhibiting stress hematopoiesis.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • SYK (Spleen tyrosine kinase)
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hydroxyurea • Tavalisse (fostamatinib)
2ms
Fostamatinib (R788), a spleen tyrosine kinase inhibitor, sensitizes pancreatic cancer cells to oncolytic vesicular stomatitis virus. (PubMed, Mol Ther Oncol)
Additionally, fostamatinib inhibited PDAC cell proliferation even in the absence of viral infection, while ruxolitinib did not. Our data suggest that fostamatinib may be repurposed as an effective drug that enhances OV therapy in PDAC by promoting OV replication and suppressing tumor growth.
Journal
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SYK (Spleen tyrosine kinase)
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Jakafi (ruxolitinib) • Tavalisse (fostamatinib)
2ms
Using Fostamatinib to Treat Post-Hematopoietic Stem Cell Transplant Immune-mediated Cytopenias (clinicaltrials.gov)
P2, N=1, Terminated, National Heart, Lung, and Blood Institute (NHLBI) | Completed --> Terminated; Clinical trial was halted prematurely due to low enrollment
Trial termination
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Tavalisse (fostamatinib)
2ms
Management of autoimmune hemolytic anemia. (PubMed, Hematology Am Soc Hematol Educ Program)
Rituximab is now the preferred second-line option for relapsed/refractory patients, comparing favorably with the traditional splenectomy. The latter is increasingly reserved for later lines together with classic immunosuppressants. Several novel treatments are in development for refractory wAIHA, encompassing drugs targeting B-cells (parsaclisib, ibrutinib, rilzabrutinib, zanubrutinib, obexelimab, ianalumab, povetacicept), plasma cells (bortezomib, daratumumab), spleen tyrosine kinase (fostamatinib, sovleplenib), and the neonatal Fc receptor (nipocalimab).
Review • Journal
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SYK (Spleen tyrosine kinase)
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Imbruvica (ibrutinib) • Rituxan (rituximab) • bortezomib • Brukinsa (zanubrutinib) • Darzalex (daratumumab) • parsaclisib (INCB50465) • Tavalisse (fostamatinib) • ianalumab (VAY736) • sovleplenib (HMPL-523)
3ms
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)
3ms
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)
3ms
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)
4ms
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)
5ms
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)
5ms
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)