Drug intelligence / Profile preview

anlotinib + irinotecan + temozolomide

Development stage
Phase 2
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Anlotinib + irinotecan + temozolomide is a combination regimen under investigation for the treatment of refractory or recurrent cancers, including neuroblastoma and high-grade gliomas. Anlotinib is a novel multi-target tyrosine kinase inhibitor that targets angiogenesis-related kinases such as fibroblast growth factor receptors (FGFR1/2/3), vascular endothelial growth factor receptors (VEGFR1/2/3), c-Kit, and Ret. It exerts anti-tumor effects by inhibiting tumor angiogenesis and proliferation through pathways like JAK2/STAT3/VEGFA. Irinotecan is a topoisomerase I inhibitor that interferes with DNA replication in cancer cells. Temozolomide is an oral alkylating agent that induces DNA damage leading to apoptosis in tumor cells. The combination aims to enhance anti-tumor efficacy via complementary mechanisms—anti-angiogenic effects from anlotinib, cytotoxicity from irinotecan and temozolomide—with evidence of synergistic activity in preclinical models and early clinical studies for difficult-to-treat tumors[1][2][3][4][5][6].

02

Targets

DNAFGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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