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fruquintinib + S-1 + raltitrexed
- Development stage
- Unknown
- Lead developer
- West China Hospital of Sichuan University
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
The RSF regimen is a combination therapy consisting of fruquintinib, S-1, and raltitrexed, currently under investigation for the treatment of refractory metastatic colorectal cancer (mCRC). S-1 is an oral fluoropyrimidine formulation containing tegafur (a 5-fluorouracil prodrug), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (an orotate phosphoribosyltransferase inhibitor that reduces gastrointestinal toxicity). Raltitrexed is a specific folate analogue inhibitor of thymidylate synthase. Fruquintinib is a highly selective oral tyrosine kinase inhibitor targeting VEGFR-1, -2, and -3. This combination therapy, evaluated in Phase II trials led by Dr. Meng Qiu at West China Hospital, aims to provide a synergistic effect by combining anti-angiogenic activity with dual-mechanism inhibition of thymidylate synthase and fluoropyrimidine-based chemotherapy.
- Other names
- Fruquintinib plus S-1 and raltitrexedFruquintinib + S-1 + raltitrexed
02
Targets
TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)OPRT (Orotidine 5'-phosphate decarboxylase)DPYD (Dihydropyrimidine dehydrogenase)
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