Drug intelligence / Profile preview

tegafur + gimeracil + oteracil

Development stage
Phase 3
Lead developer
Taiho Pharmaceutical
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tegafur + gimeracil + oteracil is an oral fixed-dose combination chemotherapy used primarily for the treatment of advanced gastric cancer and other solid tumors. Tegafur is a prodrug of fluorouracil (5-FU), a cytotoxic antimetabolite that inhibits DNA synthesis by mimicking pyrimidine and interfering with thymidylate synthase. Gimeracil inhibits dihydropyrimidine dehydrogenase (DPD), the enzyme responsible for 5-FU degradation, thereby increasing systemic exposure to 5-FU. Oteracil acts locally in the gut to inhibit orotate phosphoribosyltransferase and reduce gastrointestinal toxicity by limiting 5-FU activation in GI tissues. The combination allows for effective systemic anticancer activity with reduced GI side effects compared to traditional fluoropyrimidine therapy[1][6][9]. It is approved as first-line therapy in advanced gastric cancer (often combined with cisplatin) and has indications or clinical use in head and neck cancer, colorectal cancer, non–small-cell lung cancer, breast cancer, pancreatic cancer, biliary tract cancers[1][3][4][5].

Brand names
TS-OneTeysunoTS-One Capsule 20TS-One Capsule 25
Other names
tegafur/gimeracil/oteracil potassium combination drugS-1 Combined OD Tablets T20/T25
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)OPRT (Orotidine 5'-phosphate decarboxylase)

Beyond the preview

Go deeper on tegafur + gimeracil + oteracil.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on tegafur + gimeracil + oteracil.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call