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DRUG:

SYHA1813

i
Other names: SYHA1813
Associations
Trials
Company:
CSPC Pharma, Shanghai Inst. of Materia Medica
Drug class:
VEGFR inhibitor, CSF-1R inhibitor
Associations
Trials
2d
New P1/2 trial
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cisplatin • carboplatin • paclitaxel • everolimus • Stivarga (regorafenib) • etoposide IV • SYHA1813
7d
Relative Bioavailability and Food Effect of SYHA1813 Oral Solution in Healthy Participants (clinicaltrials.gov)
P1, N=19, Completed, Shanghai Runshi Pharmaceutical Technology Co., Ltd | Not yet recruiting --> Completed
Trial completion
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SYHA1813
5ms
Discovery of a novel BTK inhibitor S-016 and identification of a new strategy for the treatment of lymphomas including BTK inhibitor-resistant lymphomas. (PubMed, Acta Pharmacol Sin)
Among them, compound S-016 bearing a unique tricyclic structure exhibited potent BTK kinase inhibitory activity with an IC50 value of 0.5 nM, comparable to a commercially available BTK inhibitor ibrutinib (IC50 = 0.4 nM). Intriguingly, we demonstrated that SYHA1813, a compound targeting both VEGFR and CSF1R, effectively reshaped the tumor microenvironment (TME) and significantly overcame the acquired resistance to BTK inhibitors in both BTK-mutated and wild-type BTK DLBCL models by inhibiting angiogenesis and modulating macrophage polarization. Overall, this study not only promotes the development of new BTK inhibitors but also offers innovative treatment strategies for B-cell lymphomas, including those with BTK mutations.
Journal
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CSF1R (Colony stimulating factor 1 receptor)
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Imbruvica (ibrutinib) • SYHA1813
11ms
Relative Bioavailability and Food Effect of SYHA1813 Oral Solution in Healthy Participants (clinicaltrials.gov)
P1, N=18, Not yet recruiting, Shanghai Runshi Pharmaceutical Technology Co., Ltd
New P1 trial
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SYHA1813
12ms
Preclinical and early clinical studies of a novel compound SYHA1813 that efficiently crosses the blood-brain barrier and exhibits potent activity against glioblastoma. (PubMed, Acta Pharm Sin B)
SYHA1813 also displayed potent in vivo antitumor activity against GBM in immune-competent and immune-deficient mouse models, including temozolomide (TMZ) insensitive tumors. As a clinical proof of concept, SYHA1813 achieved confirmed responses in patients with recurrent GBM in an ongoing first-in-human phase I trial. The data of this study support the rationale for an ongoing phase I clinical study (ChiCTR2100045380).
Preclinical • Journal
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CSF1R (Colony stimulating factor 1 receptor)
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temozolomide • SYHA1813
over1year
A phase I dose-expansion cohort of SYHA1813, a vascular endothelial growth factor receptor (VEGFR) 1-3 /colony-stimulating factor 1 receptor (CSF1R) inhibitor, in patients (pts) with recurrent meningioma (ESMO 2023)
No grade-5 TEAEs were reported. Conclusions SYHA1813 showed encouraging objective responses with a well-tolerated safety profile in pts with recurrent meningioma.
P1 data
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FLT1 (Fms-related tyrosine kinase 1) • CSF1R (Colony stimulating factor 1 receptor)
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SYHA1813
over1year
A phase I dose-escalation study of SYHA1813, a VEGFR and CSF1R inhibitor, in patients with recurrent High-Grade Gliomas or Advanced Solid Tumors. (PubMed, Invest New Drugs)
The toxicities of SYHA1813 were manageable, and encouraging antitumor efficacy was observed in patients with recurrent malignant glioma. This study is registered with the Chinese Clinical Trial Registry ( www.chictr.org.cn/index.aspx ; identifier ChiCTR2100045380).
P1 data • Clinical Trial,Phase I • Journal • Metastases
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KDR (Kinase insert domain receptor) • CSF1R (Colony stimulating factor 1 receptor)
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SYHA1813