^
9d
FLT3-SYK inhibitor and Ixazomib combination impact HOXA and oxidative stress control by β-catenin, SQSTM1 and NRF2 in AML. (PubMed, NPJ Precis Oncol)
Dual targeting of FLT3/SYK (TAK-659) and the proteasome (Ixazomib) showed strong synergy across genetically defined AML subsets, irrespective of FLT3 mutant status. These findings define a therapeutically targetable axis linking FLT3/SYK/β-catenin signaling to stress adaptation, provide a mechanistic basis for combinatorial targeting in high-risk AML. Trial registration: NCT04079738, Date of registration 03 September 2019.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • TET2 (Tet Methylcytosine Dioxygenase 2) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C) • SQSTM1 (Sequestosome 1) • HOXA9 (Homeobox A9) • SYK (Spleen tyrosine kinase) • JUN (Jun proto-oncogene)
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FLT3-ITD mutation • FLT3 mutation • TET2 mutation
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Ninlaro (ixazomib) • mivavotinib (CB-659)
22d
Trial completion
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sovleplenib (HMPL-523)
23d
Pharmacokinetics and Bioequivalence Study of HMPL-523 Acetate Tablets in Humans (clinicaltrials.gov)
P1, N=54, Completed, Hutchmed | Recruiting --> Completed | Trial primary completion date: Feb 2026 --> Nov 2025
Trial completion • Trial primary completion date
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sovleplenib (HMPL-523)
1m
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)
2ms
New P1 trial
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sovleplenib (HMPL-523)
2ms
New P1 trial
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sovleplenib (HMPL-523)
2ms
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)
2ms
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)
3ms
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)
3ms
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)
4ms
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)
4ms
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