Thymidylate synthase — Drug Target

All drugs that target Thymidylate synthase — marketed and clinical-stage. Includes 24 drug classes acting on this target.

Drug classes

Antimetabolite; 5-fluorouracil prodrug · Antimetabolite · Fluoropyrimidine antimetabolite · Antimetabolite [EPC] · Nucleoside Metabolic Inhibitor [EPC] · doxifluridine · Vitamin C [EPC] · Antimetabolite; fluoropyrimidine combination · pyrimidine analog · Oxaliplatin analog · Antimetabolite chemotherapy combination · Antineoplastic agent

Marketed (14)

• tegafur-uracil · Yokohama City University · Antimetabolite; 5-fluorouracil prodrug · Oncology
  Tegafur-uracil is a combination prodrug that is converted to fluorouracil in the body to inhibit thymidylate synthase and disrupt DNA synthesis in cancer cells.
• Fluorouracil Injection · Suzhou Suncadia Biopharmaceuticals Co., Ltd. · Antimetabolite · Oncology
  Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• Capecitabine (Xeloda®) · National Cancer Center, Korea · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• Fudr · Antimetabolite [EPC] · Oncology
• XELODA [capecitabine] · Hoffmann-La Roche · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• Tegafur-Ugotex or Capecitabine · Liaoning Cancer Hospital & Institute · Antimetabolite; 5-fluorouracil prodrug · Oncology
  Tegafur-Uracil (Tegafur-Ugotex) is a combination prodrug that inhibits thymidylate synthase to block DNA synthesis in cancer cells.
• Xeloda · Cheplapharm · Nucleoside Metabolic Inhibitor [EPC] · Oncology
  Xeloda works by inhibiting the enzyme thymidylate synthase, which is necessary for DNA synthesis in cancer cells.
• Flutron · doxifluridine · Oncology
• Folic Acid · Pfizer · Vitamin C [EPC] · Hematology
• S-1 · TTY Biopharm · Antimetabolite; fluoropyrimidine combination · Oncology
  S-1 is an oral combination of tegafur, gimeracil, and oteracil potassium that inhibits thymidylate synthase and enhances fluorouracil activity to suppress cancer cell DNA synthesis.
• 5Fluorouracil · University of Nebraska · Antimetabolite · Oncology
  5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• Capecitabine tablets · UNICANCER · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• Metafolin · University of California, San Diego · Dermatology
• Xeloda · Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins · Oncology

Phase 3 pipeline (40)

• UFT, Calcium Folinate · Iwate Medical University · Antimetabolite · Oncology
  UFT is a prodrug that is converted into 5-fluorouracil, which inhibits thymidylate synthase, leading to DNA damage and cell death.
• STZ-5FU · Grupo Espanol de Tumores Neuroendocrinos · pyrimidine analog · Oncology
  STZ-5FU is a chemotherapeutic agent that works by interfering with DNA synthesis.
• Capecitabine(Aibin) · The First Affiliated Hospital of Henan University of Science and Technology · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• XELOXA-A · Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD) · Oxaliplatin analog · Oncology
  XELOXA-A is a chemotherapy medication used to treat cancer.
• Fluorouracil (5-FU) · EMD Serono Research & Development Institute, Inc. · Antimetabolite · Oncology
  Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• fluorouracil based chemotherapy regimens · China Medical University, China · pyrimidine analog · Oncology
  Fluorouracil is a thymidylate synthase inhibitor that disrupts DNA synthesis and function.
• Folinic Acid + 5 FU · Pfizer · Antimetabolite chemotherapy combination · Oncology
  Folinic acid enhances the cytotoxic activity of 5-fluorouracil (5-FU) by stabilizing the ternary complex between 5-FU metabolites and thymidylate synthase, thereby increasing DNA synthesis inhibition and cancer cell death.
• Maintenance Therapy with Capecitabine · Jiangxi Provincial Cancer Hospital · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• S-1 [Tegafur/Oteracil/gimeracil] · AstraZeneca · Antineoplastic agent · Oncology
  S-1 works by inhibiting thymidylate synthase, which is necessary for DNA synthesis, thereby inducing apoptosis in cancer cells.
• Carac Cream · Wake Forest University Health Sciences · Antimetabolite, topical chemotherapy · Dermatology/Oncology
  Carac Cream is a topical formulation of fluorouracil that inhibits thymidylate synthase to disrupt DNA synthesis in rapidly dividing cells, particularly actinic keratosis lesions.
• 5-Fluoruracil · Grupo Espanol Multidisciplinario del Cancer Digestivo · Antimetabolite · Oncology
  5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• Capecitabine-based chemotherapy · Ain Shams University · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell replication.
• UTD1 Injection plus capecitabine · Beijing Biostar Pharmaceuticals Co., Ltd. · Chemotherapy · Oncology
  UTD1 Injection plus capecitabine works by targeting and inhibiting the action of certain enzymes involved in DNA synthesis, thereby inhibiting cancer cell growth.
• TS-1 · National Health Research Institutes, Taiwan · Antimetabolite chemotherapy combination · Oncology
  TS-1 is an oral combination chemotherapy agent that inhibits thymidylate synthase and enhances fluorouracil activity against cancer cells.
• TS-1 (S-1) · National Cancer Center, Korea · Fluoropyrimidine antimetabolite · Oncology
  TS-1 (S-1) is an oral fluoropyrimidine combination that inhibits thymidylate synthase and other enzymes in the pyrimidine synthesis pathway to suppress tumor cell DNA synthesis.
• Capecitabine Oral Product · Abramson Cancer Center at Penn Medicine · Antimetabolite; Fluoropyrimidine · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in the body, which inhibits thymidylate synthase and disrupts DNA synthesis to kill rapidly dividing cancer cells.
• oxaliplatin , fluorouracil, and leucovorin · Sun Yat-sen University · Platinum-based chemotherapeutic agent and thymidylate synthase inhibitor · Oncology
  Oxaliplatin, fluorouracil, and leucovorin work together to inhibit thymidylate synthase and DNA synthesis, leading to cell death in rapidly dividing cancer cells.
• XELOXA · Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD) · Antimetabolite chemotherapy combination · Oncology
  XELOXA is a combination chemotherapy regimen that inhibits thymidylate synthase and DNA synthesis to kill rapidly dividing cancer cells.
• UFT adjuvant chemotherapy · Translational Research Center for Medical Innovation, Kobe, Hyogo, Japan · Antimetabolite chemotherapy · Oncology
  UFT is a combination of uracil and tegafur (a prodrug of fluorouracil) that inhibits thymidylate synthase to disrupt DNA synthesis in cancer cells.
• UFT (uracil, tegafur) · Taiho Pharmaceutical Co., Ltd. · Fluoropyrimidine antimetabolite · Oncology
  UFT is a combination of uracil and tegafur that inhibits thymidylate synthase to block DNA synthesis and induce cancer cell death.
• 5-Flurouracil · Janssen Research & Development, LLC · Antimetabolite · Oncology
  5-Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cell death.
• Placebo、5-Fluorouracil、Leucovorin · Jiangsu HengRui Medicine Co., Ltd. · Antimetabolite chemotherapy · Oncology
  5-Fluorouracil is a pyrimidine antimetabolite that inhibits thymidylate synthase and gets incorporated into RNA, disrupting nucleotide synthesis and cancer cell division, while leucovorin enhances its efficacy by stabilizing the drug-enzyme complex.
• S-1 therapy · The First Affiliated Hospital with Nanjing Medical University · Antimetabolite · Oncology
  S-1 therapy is a chemotherapy medication that works by inhibiting thymidylate synthase, thereby preventing DNA synthesis and cell division.
• S-1 Chemotherapy · Asan Medical Center · Antimetabolite · Oncology
  S-1 is a chemotherapy medication that works by inhibiting thymidylate synthase, thereby disrupting DNA synthesis and cell division.
• TAS-118 plus Oxaliplatin · Taiho Pharmaceutical Co., Ltd. · Thymidylate synthase inhibitor · Oncology
  TAS-118 is a thymidylate synthase inhibitor, and when combined with oxaliplatin, it targets rapidly dividing cancer cells.
• TEGAFUR URACIL - FOLINIC ACID · Centre Oscar Lambret · Antimetabolite · Oncology
  Tegafur uracil combined with folinic acid enhances the cytotoxic effects of 5-fluorouracil by increasing its intracellular concentration and prolonging its action.
• LV5FU2 · Centre Hospitalier Universitaire de Besancon · Antimetabolite chemotherapy combination · Oncology
  LV5FU2 is a combination chemotherapy regimen that inhibits thymidylate synthase and DNA synthesis to kill rapidly dividing cancer cells.
• continuous infusion of 5-fluorouracil · Japan Clinical Oncology Group · pyrimidine analog · Oncology
  5-fluorouracil is a thymidylate synthase inhibitor that disrupts DNA synthesis and function.
• Capecitabine monotherapy · Zhen-Hai Lu · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• Fluorouracil + folinic acid · Odense University Hospital · Antimetabolite chemotherapy combination · Oncology
  Fluorouracil inhibits thymidylate synthase to block DNA synthesis, while folinic acid enhances its cytotoxic effect by providing reduced folate cofactors.
• LV5FU2 or capecitabine · Federation Francophone de Cancerologie Digestive · Fluoropyrimidine antimetabolite · Oncology
  LV5FU2/capecitabine is a fluoropyrimidine prodrug that inhibits thymidylate synthase and gets incorporated into DNA/RNA, disrupting cancer cell replication.
• low dose capecitabine · Lund University Hospital · Antimetabolite · Oncology
  Capecitabine is a prodrug that is converted into 5-fluorouracil, which inhibits thymidylate synthase and disrupts DNA synthesis in cancer cells.
• LV5FU2 or capectitabine · Federation Francophone de Cancerologie Digestive · Fluoropyrimidine antimetabolite · Oncology
  LV5FU2 and capecitabine are fluoropyrimidine chemotherapy agents that inhibit thymidylate synthase and get incorporated into DNA/RNA to disrupt cancer cell replication.
• Fluorouracil (5FU) · University of Chicago · Antimetabolite · Oncology
  Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• Placebo + Capecitabine · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that converts to fluorouracil in tumor tissue, inhibiting thymidylate synthase to disrupt DNA synthesis and induce cancer cell death.
• UFT, Calcium Folinate, PSK · Iwate Medical University · Antineoplastic · Oncology
  UFT is a prodrug that is converted into 5-fluorouracil, a thymidylate synthase inhibitor.
• Fluorouracil/Adrucil · Bristol-Myers Squibb · Antimetabolite · Oncology
  Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase and gets incorporated into RNA and DNA, disrupting nucleotide synthesis and causing cancer cell death.
• Fluorouracil implant · Austrian Breast & Colorectal Cancer Study Group · Antimetabolite chemotherapy agent · Oncology
  Fluorouracil implant delivers the chemotherapy agent 5-fluorouracil directly to tumor tissue to inhibit thymidylate synthase and disrupt DNA synthesis in cancer cells.
• Sofetabart Mipitecan · Eli Lilly and Company · Folic acid antagonist · Oncology
  Sofetabart Mipitecan is a folic acid antagonist that inhibits thymidylate synthase.
• Tegafur-uracil (UFT) · Multicenter Clinical Study Group of Osaka, Colorectal Cancer Treatment Group · Antimetabolite · Oncology
  Tegafur-uracil (UFT) is a prodrug that is metabolized into 5-fluorouracil (5-FU), which then inhibits thymidylate synthase.

Phase 2 pipeline (12)

• 5-Fluoracil · Servicio de Salud Metropolitano Sur Oriente · pyrimidine analog · Oncology
  5-Fluorouracil is a thymidylate synthase inhibitor that disrupts DNA synthesis and function.
• ARM C FOLFIRI · GERCOR - Multidisciplinary Oncology Cooperative Group · Antimetabolite · Oncology
  Inhibits thymidylate synthase
• Capecitabine and Mitomycin C · Croatian Cooperative Group for Clinical Research in Oncology · Antineoplastic agents · Oncology
  Capecitabine is a thymidylate synthase inhibitor, and Mitomycin C is an alkylating agent.
• Intralesional 5-fluorouracil · Maharajgunj Medical Campus · Pyrimidine analog · Oncology
  Inhibits thymidylate synthase
• Fluorouracil Implants · Jiangsu Simcere Pharmaceutical Co., Ltd. · Antineoplastic · Oncology
  Fluorouracil implants work by releasing fluorouracil, a thymidylate synthase inhibitor, which interferes with DNA synthesis and function.
• Capecitabine during all Radiotherapy period · Grupo Espanol Multidisciplinario del Cancer Digestivo · Antimetabolite · Oncology
  Capecitabine is a thymidylate synthase inhibitor.
• Infusional 5-Fluorouracil · Italian Trial in Medical Oncology · Pyrimidine analog · Oncology
  Inhibits thymidylate synthase
• Capecitabine Pill · Peter MacCallum Cancer Centre, Australia · Fluoropyrimidine antimetabolite · Oncology
  Capecitabine is a prodrug that is converted to fluorouracil in tumor tissue, where it inhibits thymidylate synthase and gets incorporated into DNA and RNA to disrupt cancer cell growth.
• Fluoropyrimidine plus leucovorin · Seattle Project Corporation · Antineoplastic agent · Oncology
  Inhibits thymidylate synthase
• 5-flourouracil · AstraZeneca · pyrimidine analog · Oncology
  5-fluorouracil is a thymidylate synthase inhibitor that disrupts DNA synthesis in rapidly dividing cancer cells.
• CAPOX 3 month · NRG Oncology · Antimetabolite · Oncology
  Capecitabine is a thymidylate synthase inhibitor.
• CAPOX 6 month · NRG Oncology · Antimetabolite · Oncology
  Capecitabine is a thymidylate synthase inhibitor.

Phase 1 pipeline (1)

• 5-fluoro-2-deoxycytidine · City of Hope Medical Center · Nucleoside analog · Oncology
  Inhibits thymidylate synthase