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anlotinib + standard first-line chemotherapy

Development stage
Unknown
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Anlotinib is a novel oral small molecule multi-target tyrosine kinase inhibitor developed in China. It targets several receptor tyrosine kinases involved in tumor angiogenesis and growth, including vascular endothelial growth factor receptors (VEGFR) 1/2/3, platelet-derived growth factor receptors (PDGFR) α/β, fibroblast growth factor receptors (FGFR) 1–4, c-Kit, and Ret. Anlotinib inhibits these pathways to suppress tumor angiogenesis and proliferation. It has demonstrated efficacy as monotherapy or in combination with standard first-line chemotherapy regimens for various solid tumors such as non-small cell lung cancer (NSCLC), soft tissue sarcoma (STS), renal cell carcinoma, gastric cancer, esophageal squamous cell carcinoma, medullary thyroid carcinoma, colorectal cancer and others. In clinical trials—particularly as maintenance therapy after response to anthracycline-based chemotherapy—anlotinib has shown improved progression-free survival[2][3][4][6][7]. "Standard first-line chemotherapy" refers to established cytotoxic regimens that vary by indication; for example anthracycline-based combinations for soft tissue sarcoma or platinum-doublet regimens for NSCLC[7]. The combination is under investigation or used off-label as maintenance therapy following initial response.

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)AURKB (Aurora kinase B)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)CSF1R (Macrophage colony-stimulating factor receptor)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)DDR1 (Discoidin domain receptor 1)

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