(Gimeracil + oteracil + tegafur) is a Small Molecule owned by Taiho Pharmaceutical, and is involved in 123 clinical trials, of which 103 were completed, 17 are ongoing, and 3 are planned.

Gimeracil competitively inhibits dihydropyrimidine dehydrogenase the enzyme responsible for rapid catabolism of 5-FU into inactive metabolites leading to prolonged concentrations of 5-FU in blood. Oteracil potassium (Oxonic acid) is distributed in the gastrointestinal tract and inhibits orotate phosphoribosyl-transferase (OPRT) which converts 5-FU to 5-fluorouridine 5’-monophosphate thereby decreasing activation of 5-FU in the gut and activated 5-FU-related gastrointestinal toxicity.Tegafur is a congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme. Subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by inhibiting thymidylate synthase and reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate.

The revenue for (Gimeracil + oteracil + tegafur) is expected to reach a total of $373m through 2038. This change impacts the valuation of this asset and is an important factor to understand the current value of the drug in a clinical process. View the complete picture with the (Gimeracil + oteracil + tegafur) NPV Report.

(Gimeracil + oteracil + tegafur) is currently owned by Taiho Pharmaceutical. Otsuka Holdings is the other company associated in development or marketing of (Gimeracil + oteracil + tegafur).

(Gimeracil + oteracil + tegafur) Overview

Gimeracil, Oteracil, Tegafur (Teysuno/TS-1) is a fixed dose combination acts as an anti-metabolite preparation. It is formulated as hard gelatin capsules and granules for oral route of administration. It is indicated in adults for the treatment of advanced gastric cancer, biliary cancer, colorectal cancer, head and neck cancer, non-small cell lung cancer, inoperable or relapsed breast cancer, and pancreatic cancer, when given in combination with cisplatin. TS-1 is under development for the treatment of metastatic pancreatic cancer and resected adenocarcinoma pancreatic cancer.

It was also under development for the treatment of non-small cell lung cancer, hepatocellular carcinoma, uterocervicall cancer and renal cell carcinoma, pancreatic ductal adenocarcinoma and colorectal cancer (as an adjuvant therapy).

Otsuka Holdings Overview

Otsuka Holdings (Otsuka) is a holding company, which operates various businesses such as pharmaceuticals, nutraceuticals, consumer products and other businesses through its subsidiaries. It focuses on the research and development, manufacture, and sale of medicines for the treatment of cancer, cardiovascular diseases, central nervous system disorders, ophthalmic diseases, gastrointestinal and respiratory diseases, infectious diseases, dermatological conditions and allergies. The company’s product portfolio includes pharmaceutical products, cosmetics, functional foods and beverages, alcoholic beverages, fine chemicals, electronic equipment, functional chemicals, medical devices and OTC products. It markets its products in North America, Europe, and Asia. Otsuka is headquartered in Chiyoda-ku, Tokyo, Japan.

The company reported revenues of (Yen) JPY1,498,276 million for the fiscal year ended December 2021 (FY2021), an increase of 5.3% over FY2020. In FY2021, the company’s operating margin was 10.3%, compared to an operating margin of 13.8% in FY2020. In FY2021, the company recorded a net margin of 8.4%, compared to a net margin of 10.4% in FY2020. The company reported revenues of JPY451,811 million for the third quarter ended September 2022, an increase of 4.1% over the previous quarter.

Quick View – (Gimeracil + oteracil + tegafur)

Report Segments
  • Innovator (Non-NME)
Drug Name
  • (Gimeracil + oteracil + tegafur)
Administration Pathway
  • Oral
Therapeutic Areas
  • Oncology
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Highest Development Stage
  • Marketed

GlobalData, the leading provider of industry intelligence, provided the underlying data, research, and analysis used to produce this article.

To create this model, GlobalData takes into account factors including patent law, known and projected regulatory approval processes, cash flows, potential applicable patients, drug margins, company expenses, and pricing estimates. Combining these data points with GlobalData’s world class analysis creates high value models that companies can use to help in evaluation processes for each drug or company.

The rNPV method integrates the probability of a drug reaching a clinical stage into the cash flow at that time, which provides a more accurate rNPV, as it considers the probability that the drug never makes it through the clinical pathway to commercialization. GlobalData’s rNPV model uses proprietary likelihood of approval (LoA)and phase transition success rate(PTSR) data for the indication in the highest development stage, which can be found on GlobalData’s Pharmaceutical Intelligence Center.