Drug intelligence / Profile preview

apatinib + oxaliplatin + tegafur + gimeracil + oteracil potassium

Development stage
Unknown
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Apatinib + oxaliplatin + tegafur + gimeracil + oteracil potassium is a combination neoadjuvant therapy being evaluated for the treatment of locally advanced gastric cancer. This regimen combines apatinib, a selective small-molecule tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor 2 (VEGFR-2) to inhibit tumor angiogenesis, with the SOX chemotherapy regimen. SOX consists of oxaliplatin, a platinum-based agent that forms DNA cross-links to inhibit DNA replication, and S-1, an oral fluoropyrimidine. S-1 is a three-component drug containing tegafur (a prodrug of the antimetabolite 5-fluorouracil), gimeracil (which inhibits the degradation of 5-fluorouracil), and oteracil potassium (which reduces gastrointestinal toxicity). This combination is primarily being studied in clinical trials led by Professor Chang-Ming Huang at Fujian Medical University Union Hospital to improve resectability and pathological complete response rates in gastric cancer patients.

Other names
apatinib + SOXapatinib + S-1 + oxaliplatin
02

Targets

DNADPYD (Dihydropyrimidine dehydrogenase)OPRT (Orotidine 5'-phosphate decarboxylase)RET (Rearranged during transfection receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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