Drug intelligence / Profile preview

tegafur + gimeracil + oteracil potassium + cisplatin + everolimus

Development stage
Unknown
Lead developer
National University Hospital
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

TS-ONE + cisplatin + RAD001 is an investigational combination therapy regimen being evaluated for the treatment of refractory solid malignancies, including gastric cancer. The regimen consists of three primary components: TS-1 (a fixed-dose combination of the 5-fluorouracil prodrug tegafur, the dihydropyrimidine dehydrogenase inhibitor gimeracil, and the orotate phosphoribosyltransferase inhibitor oteracil potassium), the platinum-based cytotoxic agent cisplatin, and the mTOR inhibitor everolimus (RAD001). The combination aims to leverage the synergistic effects of mTOR inhibition with traditional chemotherapy to overcome treatment resistance and improve clinical outcomes in patients who have failed prior therapies. Preclinical data suggests that the addition of everolimus can sensitize tumor cells to cisplatin and fluoropyrimidines by inhibiting survival pathways frequently upregulated in resistant cancers.

Brand names
TeysunoAfinitor
Other names
TS-ONE + cisplatin + RAD001S-1 + cisplatin + everolimusTS-1 + CDDP + everolimus
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)mTOR (Mammalian target of rapamycin kinase)DNAOPRT (Orotidine 5'-phosphate decarboxylase)

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