Ts-1 (Teysuno, S-1)

Other Medications · Approved since 2010

US FDA Approved Oral 4 Clinical Trials
Thymidylate synthase dihydropyrimidine dehydrogenase

Description

TS-1 (tegafur/gimeracil/oteracil) is an oral fluoropyrimidine-based chemotherapy agent that combines three active components to enhance antitumor efficacy while reducing toxicity. It is used as both first-line and second-line treatment for advanced and metastatic colorectal cancer, often in combination with other agents such as irinotecan or oxaliplatin. The formulation provides sustained 5-fluorouracil levels through tegafur while gimeracil inhibits 5-FU degradation and oteracil reduces gastrointestinal toxicity.

Mechanism of Action

TS-1 works through its primary component tegafur, which is converted to 5-fluorouracil (5-FU) in tumor tissues, where it inhibits thymidylate synthase and disrupts DNA synthesis and repair. Gimeracil inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU catabolism, thereby maintaining therapeutic drug levels. Oteracil selectively inhibits 5-FU phosphorylation in the gastrointestinal tract, reducing dose-limiting diarrhea and mucositis.

Molecular Targets

Side Effects

Diarrhea Nausea Vomiting Fatigue Hand-foot syndrome Stomatitis Decreased appetite Neutropenia

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT01269216 Phase 2
Archived
A Study of Neoadjuvant Chemoradiotherapy With 5-FU/Leucovorin (FL) vs. TS-1/Irinotecan in Patients With Locally Advanced Rectal Cancer
South Korea
NCT00531245 Phase 1
Archived
A Phase I/II Trial of TS-1 and Oxaliplatin in Patients With Advanced Colorectal Cancer
South Korea
NCT00316745 Phase 3
Suspended
IRIS Followed by mFOLFOX6 or the Reverse Sequence in Advanced Colorectal Cancer
Japan
NCT00284258 Phase 2
Archived
Phase II/III Trial of CPT-11/5-FU/l-LV Versus CPT-11/TS-1 as Second Line Chemotherapy of Unresectable Colorectal Cancer
Japan