Drug intelligence / Profile preview

zanzalintinib

Development stage
Phase 3
Lead developer
Exelixis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Zanzalintinib is an orally bioavailable, next-generation small molecule tyrosine kinase inhibitor (TKI) that targets multiple receptor tyrosine kinases implicated in tumor angiogenesis, metastasis, and immunosuppression. Its primary molecular targets include hepatocyte growth factor receptor (c-Met; HGFR), vascular endothelial growth factor receptor type 2 (VEGFR2), and the TAM family kinases AXL and MER. By inhibiting these kinases, zanzalintinib blocks key signaling pathways involved in tumor cell proliferation, survival, invasion, angiogenesis, metastasis, and immune evasion. This results in antiangiogenic and antineoplastic effects as well as modulation of the tumor immune microenvironment. Zanzalintinib is being developed by Exelixis for use primarily in advanced or metastatic renal cell carcinoma—including both clear cell (ccRCC) and non-clear-cell subtypes—as well as colorectal cancer (CRC) and squamous cell carcinoma of the head and neck (SCCHN). It is currently under investigation in phase 3 clinical trials both as monotherapy and in combination with immune checkpoint inhibitors[1][2][4][5][6][7].

Brand names
Zanzalintinib
Other names
zanzalintinib
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)AXL (AXL receptor tyrosine kinase)MERTK (MER proto-oncogene, tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)

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