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Tegafur

Tegafur is an oral chemotherapy drug being investigated in various clinical trials for treating different types of cancer. As a prodrug of 5-fluorouracil (5-FU), tegafur is often combined with other medications to enhance its effectiveness and reduce side effects. This article summarizes key findings from recent clinical trials exploring tegafur’s potential in cancer treatment.

Table of Contents

What is Tegafur?

Tegafur is an anticancer drug that belongs to a class of medications called fluoropyrimidines. It is often referred to by its brand names, which include UFT and S-1[1]. Tegafur is a prodrug, which means it is converted into an active form of the medication called 5-fluorouracil (5-FU) in the body[2].

Conditions Treated with Tegafur

Tegafur is used to treat various types of cancer, including:

  • Colorectal cancer: Cancer that starts in the colon or rectum[1]
  • Esophageal squamous cell carcinoma: A type of cancer that affects the esophagus (the tube that connects the throat to the stomach)[3]
  • Head and neck cancer: Cancers that start in the mouth, nose, throat, or nearby areas[2]
  • Hepatocellular carcinoma: The most common type of liver cancer[4]
  • Gallbladder carcinoma: Cancer that begins in the gallbladder[5]
  • Extrapancreatic neuroendocrine tumors: Rare tumors that develop in hormone-producing cells outside the pancreas[6]

How Tegafur Works

Tegafur works by interfering with the growth of cancer cells. Once it’s converted to 5-FU in the body, it inhibits an enzyme called thymidylate synthase (TS). This enzyme is crucial for DNA synthesis, which cancer cells need to grow and divide. By blocking TS, Tegafur helps to slow down or stop the growth of cancer cells[2].

How Tegafur is Administered

Tegafur is typically given orally (by mouth) in the form of capsules or tablets. The dosage and schedule can vary depending on the specific condition being treated and other factors. Some common administration methods include:

  • Daily dosing: For example, 300 mg/m² three times a day[1]
  • Twice daily dosing: Such as 40-60 mg twice a day for 14 days in a 21-day cycle[6]
  • Dosing based on body surface area: For instance, 40 mg for body surface area <1.25m², 50 mg for 1.25-1.5m², and 60 mg for >1.5m²[7]

Tegafur in Combination Therapies

Tegafur is often used in combination with other medications to enhance its effectiveness. Some common combinations include:

  • Tegafur + Uracil (UFT): This combination helps to maintain higher levels of the active drug in the body[4]
  • Tegafur + Folinic acid: Folinic acid can enhance the effects of Tegafur[1]
  • Tegafur + Oxaliplatin (SOX regimen): Used in treating various gastrointestinal cancers[5]
  • Tegafur + Temozolomide: Used in treating neuroendocrine tumors[6]
  • Tegafur + Immunotherapy drugs: Such as Adebrelimab and Apatinib, used in advanced esophageal cancer[7]

Ongoing Clinical Trials

Several clinical trials are currently exploring new ways to use Tegafur, including:

  • As maintenance therapy after surgery for stage III colon cancer[8]
  • In combination with immunotherapy for advanced esophageal cancer[7]
  • As part of a metronomic chemotherapy regimen for head and neck cancer[2]

Potential Side Effects

Like all medications, Tegafur can cause side effects. Some potential side effects include:

  • Diarrhea
  • Nausea and vomiting
  • Decreased appetite
  • Fatigue
  • Bone marrow suppression (which can lead to increased risk of infections, anemia, or bleeding)
  • Liver function abnormalities

It’s important to note that not everyone experiences these side effects, and your healthcare provider will monitor you closely during treatment[4][2].

Cancer Type Trial Combination Key Findings/Objectives
Esophageal Squamous Cell Carcinoma Tegafur + Tislelizumab Investigating efficacy and safety in patients with residual primary lesions after neoadjuvant therapy and surgery
Stage II Colon Cancer Tegafur-Uracil Assessing 3-year disease-free survival and safety profile in MSI-L or MSS patients
Oral Cavity Cancer Tegafur-Uracil Evaluating 2-year distant failure rate in patients with extracapsular spreading of lymph nodes
Stage III Colon Cancer Tegafur-Uracil + Oxaliplatin Comparing 3-year disease-free survival with observation following adjuvant oxaliplatin-based regimen
Head and Neck Cancer Tegafur-Uracil Investigating metronomic chemotherapy approach for locally advanced squamous cell carcinoma
Gallbladder Carcinoma Tegafur + Oxaliplatin + Apatinib Evaluating progression-free survival in advanced cases
Extrapancreatic Neuroendocrine Tumor Tegafur + Temozolomide +/- Thalidomide Assessing objective response rate and other efficacy measures in advanced cases
Hepatocellular Carcinoma Tegafur-Uracil + Thalidomide Evaluating overall response rate and disease stabilization in advanced or metastatic cases

FAQ

  • What types of cancer is tegafur being studied for? Tegafur is being investigated for several cancer types, including esophageal squamous cell carcinoma, colon cancer, oral cavity cancer, head and neck cancer, gallbladder carcinoma, and hepatocellular carcinoma.
  • How is tegafur typically administered? Tegafur is usually given orally, often in combination with other drugs. The dosage and schedule can vary depending on the specific trial and cancer type being treated.
  • What are some common drugs combined with tegafur in clinical trials? Tegafur is often combined with drugs like uracil (forming UFT or UFUR), oxaliplatin, tislelizumab, apatinib, temozolomide, and thalidomide in various clinical trials.
  • What are some potential benefits of tegafur compared to traditional chemotherapy? As an oral medication, tegafur offers greater convenience for patients. It may also have a more favorable side effect profile compared to intravenous chemotherapy in some cases.
  • Are there any notable side effects associated with tegafur? While specific side effects can vary, tegafur may cause issues like bone marrow depression, liver dysfunction, dehydration, anorexia, nausea, and vomiting. Close monitoring is typically required during treatment.

Ongoing Clinical Trials on Tegafur

  • Study Comparing Chemotherapy with Irinotecan, Folinic Acid, and Oxaliplatin for Patients with Locally Recurrent Rectal Cancer

    Recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Belgium The Netherlands Norway Portugal Sweden

  • Study on Using ctDNA to Guide Treatment in Patients with Metastatic Colorectal Cancer Using Oxaliplatin, Capecitabine, Calcium Folinate, Irinotecan, and Fluorouracil

    Recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    Denmark Germany Norway

  • Study of pembrolizumab, capecitabine, or olaparib in patients with early-stage triple negative breast cancer and remaining disease after initial treatment

    Not yet recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    The Netherlands

  • Study of Irinotecan with S1 or 5-Fluorouracil for Patients with Metastatic Pancreatic Cancer After Gemcitabine Treatment

    Not recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    Austria Italy The Netherlands Spain

  • Study on Rilvegostomig and Chemotherapy for Patients with Biliary Tract Cancer After Surgery

    Not recruiting

    1 1 1
    Investigated diseases:
    Investigated drugs:
    Belgium Denmark France Germany Italy Norway +2

  • Study on the Impact of DPYD Gene Test on the Safety and Efficacy of Fluorouracil, Capecitabine, and Tegafur in Finnish Patients with Breast or Colon Cancer

    Not recruiting

    1 1 1 1
    Investigated diseases:
    Investigated drugs:
    Finland

Glossary

  • Tegafur: An oral chemotherapy drug that is a prodrug of 5-fluorouracil (5-FU), used in the treatment of various types of cancer.
  • Prodrug: A medication that is administered in an inactive form and then metabolized in the body to produce the active drug.
  • 5-Fluorouracil (5-FU): A chemotherapy drug that interferes with DNA synthesis and cell division, commonly used to treat various cancers.
  • Uracil: A compound often combined with tegafur to inhibit its breakdown, allowing for more sustained levels of the active drug in the body.
  • Metronomic chemotherapy: A method of administering chemotherapy drugs in lower, more frequent doses to reduce side effects and potentially improve effectiveness.
  • Adjuvant therapy: Additional cancer treatment given after the primary treatment to lower the risk of cancer recurrence.
  • Progression-free survival (PFS): The length of time during and after treatment that a patient lives with cancer without it worsening.
  • Overall survival (OS): The length of time from the start of treatment or diagnosis that patients are still alive.
  • Objective response rate (ORR): The proportion of patients whose cancer shrinks or disappears after treatment.
  • Disease control rate (DCR): The percentage of patients with advanced or metastatic cancer who have achieved complete response, partial response, and stable disease.

References

  1. https://clinicaltrials.gov/study/NCT00905047
  2. https://clinicaltrials.gov/study/NCT00855881
  3. https://clinicaltrials.gov/study/NCT06354140
  4. https://clinicaltrials.gov/study/NCT01539018
  5. https://clinicaltrials.gov/study/NCT03702491
  6. https://clinicaltrials.gov/study/NCT03204032
  7. https://clinicaltrials.gov/study/NCT06339619
  8. https://clinicaltrials.gov/study/NCT02836977