Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C5H4ClNO2 |
| Molecular Weight | 145.544 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC1=CC(=O)NC=C1Cl
InChI
InChIKey=ZPLQIPFOCGIIHV-UHFFFAOYSA-N
InChI=1S/C5H4ClNO2/c6-3-2-7-5(9)1-4(3)8/h1-2H,(H2,7,8,9)
| Molecular Formula | C5H4ClNO2 |
| Molecular Weight | 145.544 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including, www.ncbi.nlm.nih.gov/pubmed/24014883
Curator's Comment: description was created based on several sources, including, www.ncbi.nlm.nih.gov/pubmed/24014883
Gimeracil is a component of an oral fixed combination known under the name Teysuno or S-1 (tegafur, gimeracil and oteracil potassium at a molar ratio of 1:0.4:1). The formulation was approved in Asia and Europe for the treatment of a rare condition of gastric cancer. Given in combination, gimeracil enhances the efficacy of tegafur by inhibiting dihydropyrimidine dehydrogenase, an enzyme involved in metabolism of tegafur and its active metabolite 5-fluorouracil.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
452 ng/mL |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
305 ng/mL |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1884 ng × h/mL |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1483 ng × h/mL |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
3 mg × h/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/14650374 |
12.08 mg single, oral dose: 12.08 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.6 h |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
67.8% |
14.5 mg single, oral dose: 14.5 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
Other AEs: Leucopenia, Neutropenia... Other AEs: Leucopenia (grade 3-5, 1.7%) Sources: Neutropenia (grade 3-5, 6.7%) Febrile neutropenia (grade 3-5, 1.1%) Anaemia (grade 3-5, 2.8%) Thrombocytopenia (grade 3-5, 1.7%) Stomatitis (grade 3-5, 3.4%) Nausea (grade 3-5, 1.4%) Vomiting (grade 3-5, 2%) Decreased appetite (grade 3-5, 9.8%) Diarrhoea (grade 3-5, 8.4%) Constipation (grade 3-5, 0.8%) Maculopapular rash (grade 3-5, 1.4%) Weight loss (grade 3-5, 0.6%) Dyspnea (grade 3-5, 0.6%) |
25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Nausea, Fatigue... Other AEs: Nausea (all grades, 35%) Sources: Fatigue (all grades, 32%) Diarrhoea (all grades, 30%) Vomiting (all grades, 17%) Anorexia (all grades, 18%) Rash (all grades, 17%) Diarrhoea (grade 3-5, 9.6%) Nausea (grade 3-5, 2.5%) Vomiting (grade 3-5, 2.5%) Abdominal pain (grade 3-5, 2.5%) Stomatitis (grade 3-5, 1.9%) Dehydration (grade 3-5, 5.1%) |
25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Anorexia, Hyponatraemia... Other AEs: Anorexia (grade 3-4, 12.4%) Sources: Hyponatraemia (grade 3-4, 5.2%) Nausea (grade 3-4, 5.6%) Neutrophil count decreased (grade 3-4, 5.6%) Anaemia (grade 3-4, 12.8%) Leucopenia (grade 3-4, 0.9%) Neutropenic infection (grade 3-4, 0.4%) |
40 mg/m2 2 times / day steady, oral Dose: 40 mg/m2, 2 times / day Route: oral Route: steady Dose: 40 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Dyspnea | grade 3-5, 0.6% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Weight loss | grade 3-5, 0.6% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Constipation | grade 3-5, 0.8% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Febrile neutropenia | grade 3-5, 1.1% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Maculopapular rash | grade 3-5, 1.4% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Nausea | grade 3-5, 1.4% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Leucopenia | grade 3-5, 1.7% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Thrombocytopenia | grade 3-5, 1.7% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Vomiting | grade 3-5, 2% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Anaemia | grade 3-5, 2.8% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Stomatitis | grade 3-5, 3.4% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Neutropenia | grade 3-5, 6.7% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Diarrhoea | grade 3-5, 8.4% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Decreased appetite | grade 3-5, 9.8% | 80 mg 1 times / day steady, oral Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 65 years (range: 23–85 years) Health Status: unhealthy Age Group: 65 years (range: 23–85 years) Sources: |
| Rash | all grades, 17% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Vomiting | all grades, 17% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Anorexia | all grades, 18% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Diarrhoea | all grades, 30% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Fatigue | all grades, 32% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Nausea | all grades, 35% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Stomatitis | grade 3-5, 1.9% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Abdominal pain | grade 3-5, 2.5% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Nausea | grade 3-5, 2.5% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Vomiting | grade 3-5, 2.5% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Dehydration | grade 3-5, 5.1% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Diarrhoea | grade 3-5, 9.6% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Neutropenic infection | grade 3-4, 0.4% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Leucopenia | grade 3-4, 0.9% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Anorexia | grade 3-4, 12.4% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Anaemia | grade 3-4, 12.8% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Hyponatraemia | grade 3-4, 5.2% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Nausea | grade 3-4, 5.6% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Neutrophil count decreased | grade 3-4, 5.6% | 25 mg/m2 2 times / day multiple, oral Recommended Dose: 25 mg/m2, 2 times / day Route: oral Route: multiple Dose: 25 mg/m2, 2 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Proteomic differential display analysis for TS-1-resistant and -sensitive pancreatic cancer cells using two-dimensional gel electrophoresis and mass spectrometry. | 2011-06 |
|
| Chemosensitivity test for 5-fluorouracil and 5-chloro-2, 4-dihydroxypyridine predicts outcome of gastric cancer patients receiving S-1 postoperatively. | 2010-11 |
|
| An early phase II trial of S-1 in Japanese patients with cytokine-refractory metastatic renal cell carcinoma. | 2010-11 |
|
| Gemcitabine and s-1 combination chemotherapy in patients with advanced biliary tract cancer: a retrospective study. | 2010-09 |
|
| Can the 2-(13)C-uracil breath test be used to predict the effect of the antitumor drug S-1? | 2010-07 |
|
| N(3)-o-toluyl-fluorouracil inhibits human hepatocellular carcinoma cell growth via sustained release of 5-FU. | 2010-05 |
|
| A Phase II Study of S-1 Monotherapy as a First-line Combination Therapy of S-1 Plus Cisplatin as a Second-line Therapy, and Weekly Paclitaxel Monotherapy as a Third-line Therapy in Patients with Advanced Gastric Carcinoma: A Second Report. | 2010-03-24 |
|
| [Construction of a system for proper TS-1 application]. | 2010-03 |
|
| Two dosages of oral fluoropyrimidine S-1 of 35 and 40 mg/m2 bid: comparison of the pharmacokinetic profiles in Korean patients with advanced gastric cancer. | 2010-01 |
|
| S-1 mediates the inhibition of lymph node metastasis in oral cancer cells. | 2009-10 |
|
| Analysis of feasibility and toxicity of concurrent chemoradiotherapy with S-1 for locally advanced squamous cell carcinoma of the head and neck in elderly cases and/or cases with comorbidity. | 2009-10 |
|
| Phase II trial of S-1 and cisplatin with concurrent radiotherapy for locally advanced non-small-cell lung cancer. | 2009-07-21 |
|
| High Ki67, Bax, and thymidylate synthase expression well correlates with response to chemoradiation therapy in locally advanced rectal cancers: proposal of a logistic model for prediction. | 2009-07-07 |
|
| Pharmacokinetics of 5-fluorouracil in elderly Japanese patients with cancer treated with S-1 (a combination of tegafur and dihydropyrimidine dehydrogenase inhibitor 5-chloro-2,4-dihydroxypyridine). | 2009-07 |
|
| Phase I study of the sequential administration of S-1 and cisplatin for metastatic gastric cancer. | 2009-05 |
|
| Fixed dosing and pharmacokinetics of S-1 in Japanese cancer patients with large body surface areas. | 2009-05 |
|
| Development history and concept of an oral anticancer agent S-1 (TS-1): its clinical usefulness and future vistas. | 2009-01 |
|
| Successful treatment of advanced gallbladder cancer with an anticancer drug S-1: assessment based on intratumoral gene. | 2008-12 |
|
| High intratumoral dihydropyrimidine dehydrogenase mRNA levels in pancreatic cancer associated with a high rate of response to S-1. | 2008-12 |
|
| [Case report of gastric cancer patient who suffered life-threatening adverse events including severe myelosuppression during neoadjuvant chemotherapy with S-1 and CDDP combination]. | 2008-09 |
|
| A randomised multicentre phase II trial of capecitabine vs S-1 as first-line treatment in elderly patients with metastatic or recurrent unresectable gastric cancer. | 2008-08-19 |
|
| Anti-angiogenic effect of 5-Fluorouracil-based drugs against human colon cancer xenografts. | 2008-08-18 |
|
| Combination therapy of S-1 with selective cyclooxygenase-2 inhibitor for liver metastasis of colorectal carcinoma. | 2008-05-30 |
|
| CYP2A6 and the plasma level of 5-chloro-2, 4-dihydroxypyridine are determinants of the pharmacokinetic variability of tegafur and 5-fluorouracil, respectively, in Japanese patients with cancer given S-1. | 2008-05 |
|
| Phase I/II study of oxaliplatin with oral S-1 as first-line therapy for patients with metastatic colorectal cancer. | 2008-03-25 |
|
| S-1 monotherapy as a neoadjuvant treatment for locally advanced gastric cancer. | 2008-03 |
|
| Synergistic antitumor effect of combined 5-fluorouracil (5-FU) with 5-chloro-2,4-dihydroxypyridine on 5-FU-resistant gastric cancer cells: possible role of a dihydropyrimidine dehydrogenase-independent mechanism. | 2007-10 |
|
| Alteration of dihydropyrimidine dehydrogenase expression by IFN-alpha affects the antiproliferative effects of 5-fluorouracil in human hepatocellular carcinoma cells. | 2007-08 |
|
| A phase I trial of S-1 with concurrent radiotherapy for locally advanced pancreatic cancer. | 2007-06-04 |
|
| Phase-I trial of oral fluoropyrimidine anticancer agent (S-1) with concurrent radiotherapy in patients with unresectable pancreatic cancer. | 2007-05-07 |
|
| [Successful low-dose TS-1 administration in an elderly colon cancer patient with liver metastasis]. | 2007-04 |
|
| The significance of the expression of dihydropyrimidine dehydrogenase in prostate cancer. | 2007-03 |
|
| Correlation between the urinary dihydrouracil-uracil ratio and the 5-FU plasma concentration in patients treated with oral 5-FU analogs. | 2006-11-11 |
|
| Potassium oxonate, an enzyme inhibitor compounded in S-1, reduces the suppression of antitumor immunity induced by 5-fluorouracil. | 2006-08 |
|
| Phase II trial of oral S-1 combined with gemcitabine in metastatic pancreatic cancer. | 2006-06-05 |
|
| [Combination chemotherapy with S-1 and cisplatin for non-small cell lung cancer]. | 2006-06 |
|
| [Pharmacokinetics of S-1]. | 2006-06 |
|
| Phase I/II study of S-1 combined with irinotecan for metastatic advanced gastric cancer. | 2006-04-24 |
|
| DNA methylation of CHFR is not a predictor of the response to docetaxel and paclitaxel in advanced and recurrent gastric cancer. | 2006-02-16 |
|
| Enhancement of the anti-tumor activity of S-1 by low-dose cisplatin in mice bearing the sarcoma-180 model. | 2005-11 |
|
| Randomized scheduling feasibility study of S-1 for adjuvant chemotherapy in advanced head and neck cancer. | 2005-10-17 |
|
| [A trial of TS-1 administration on the basis of the pharmacokinetic study for an advanced gastric cancer patient with impaired renal function]. | 2005-10 |
|
| The role of thymidylate synthase and dihydropyrimidine dehydrogenase in resistance to 5-fluorouracil in human lung cancer cells. | 2005-09 |
|
| Role of dihydropyrimidine dehydrogenase inhibitory fluoropyrimidine against non-small cell lung cancer--in correlation with the tumoral expression of thymidylate synthase and dihydropyrimidine dehydrogenase. | 2005-07 |
|
| Correlations between antitumor activities of fluoropyrimidines and DPD activity in lung tumor xenografts. | 2005-07 |
|
| Phase I trial of oral S-1 combined with gemcitabine in metastatic pancreatic cancer. | 2005-06-20 |
|
| Phase II study of S-1 in patients with advanced biliary tract cancer. | 2004-11-15 |
|
| Thymidylate synthase predictive power is overcome by irinotecan combination therapy with S-1 for gastric cancer. | 2004-10-04 |
|
| Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation. | 2004-08-16 |
|
| Safety and efficacy of S-1, a novel oral fluorouracil antitumor drug, for a chronic renal failure patient maintained on hemodialysis. | 2004 |
Sample Use Guides
The recommended dose of gimeracil is 10 mg/m2 (as a part of oral combination consisting of tegafur, gimeracil and oteracil potassium at a molar ratio of 1:0.4:1) twice a day, for 21 consecutive days followed by 7 days rest.
Route of Administration:
Oral
TE-5 and TE-5R cells were plated in a 96-well plate and cultured for 24 h, and then they were treated with the indicated concentrations of 5-FU in the presence of gimeracil for 72 h at a molar ratio of 1:0.2 (5-FU:gimeracil). IC50 values with and without gimeracil in TE-5 cells were 4.9 and 4.8 uM, respectively, and those in TE-5R cells were 20.8 and 59.0 uM, respectively.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:18:58 GMT 2025
by
admin
on
Mon Mar 31 18:18:58 GMT 2025
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| Record UNII |
UA8SE1325T
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| Record Status |
Validated (UNII)
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| Record Version |
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FDA ORPHAN DRUG |
225006
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EMA ASSESSMENT REPORTS |
TEYSUNO (AUTHORIZED: STOMACH NEOPLASMS)
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NCI_THESAURUS |
C2019
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UA8SE1325T
Created by
admin on Mon Mar 31 18:18:58 GMT 2025 , Edited by admin on Mon Mar 31 18:18:58 GMT 2025
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