Drug intelligence / Profile preview

tegafur + apatinib

Development stage
Unknown
Lead developer
Jiangsu Hengrui Medicine
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tegafur + apatinib is an investigational combination therapy consisting of two small molecule drugs used primarily in the treatment of advanced cancers, particularly gastric cancer and esophageal squamous cell carcinoma. Tegafur is a prodrug of 5-fluorouracil (5-FU), functioning as an antimetabolite chemotherapeutic agent that inhibits DNA synthesis by interfering with thymidylate synthase. Apatinib is a selective inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), acting as an antiangiogenic agent to block tumor blood vessel formation. The combination aims to leverage the cytotoxic effects of tegafur with the antiangiogenic properties of apatinib, resulting in improved response rates and progression-free survival compared to monotherapy, though it may also increase adverse events and impact quality of life[2][3][7].

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)TS (Thymidylate synthase)

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