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)
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 |
|---|---|---|---|---|
374.9 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23289150 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3 mg × h/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/14650374 |
25 mg/m² single, oral dose: 25 mg/m² 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 |
|---|---|---|---|---|
7.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23289150 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: TEGAFUR |
GIMERACIL unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
67.8% |
GIMERACIL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
Other AEs: Nausea, Fatigue... Other AEs: Nausea (all grades, 35%) Sources: Page: p.53Fatigue (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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
Other AEs: Anorexia, Hyponatraemia... Other AEs: Anorexia (grade 3-4, 12.4%) Sources: Page: p.53Hyponatraemia (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 Co-administed with:: tegafur Sources: oteracil |
unhealthy, adult Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Dyspnea | grade 3-5, 0.6% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Weight loss | grade 3-5, 0.6% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Constipation | grade 3-5, 0.8% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Febrile neutropenia | grade 3-5, 1.1% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Maculopapular rash | grade 3-5, 1.4% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Nausea | grade 3-5, 1.4% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Leucopenia | grade 3-5, 1.7% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Thrombocytopenia | grade 3-5, 1.7% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Vomiting | grade 3-5, 2% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Anaemia | grade 3-5, 2.8% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Stomatitis | grade 3-5, 3.4% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Neutropenia | grade 3-5, 6.7% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Diarrhoea | grade 3-5, 8.4% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 Sources: |
| Decreased appetite | grade 3-5, 9.8% | 80 mg 1 times / day steady, oral (typical) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Co-administed with:: tegafur Sources: oteracil |
unhealthy, 65 years (range: 23–85 years) n = 358 Health Status: unhealthy Condition: cell lung cancer Age Group: 65 years (range: 23–85 years) Population Size: 358 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 11 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 11 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
| 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 Co-administed with:: tegafur Sources: Page: p.53oteracil |
unhealthy, adult n = 700 Health Status: unhealthy Condition: advanced gastric cancer Age Group: adult Population Size: 700 Sources: Page: p.53 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [New oral anticancer drug, TS-1 (S-1)--from bench to clinic]. | 2001 Jun |
|
| Effects of 5-fluorouracil on the drug-metabolizing enzymes of the small intestine and the consequent drug interaction with nifedipine in rats. | 2001 Jun |
|
| Involvement of microsomal cytochrome P450 and cytosolic thymidine phosphorylase in 5-fluorouracil formation from tegafur in human liver. | 2001 Mar |
|
| Possible regulation of 5-fluorouracil-induced neuro- and oral toxicities by two biochemical modulators consisting of S-1, a new oral formulation of 5-fluorouracil. | 2001 May-Jun |
|
| Clinical studies of three oral prodrugs of 5-fluorouracil (capecitabine, UFT, S-1): a review. | 2002 |
|
| Prognostic significance of dihydropyrimidine dehydrogenase expression in breast cancer. | 2002 Jan 21 |
|
| A novel mutant allele of the CYP2A6 gene (CYP2A6*11 ) found in a cancer patient who showed poor metabolic phenotype towards tegafur. | 2002 Jun |
|
| S-1 in gastric cancer: a comprehensive review. | 2003 |
|
| Correlation between 5-fluorouracil metabolism and treatment response in two variants of C26 murine colon carcinoma. | 2003 Aug 18 |
|
| Phase I/II study of S-1 combined with cisplatin in patients with advanced gastric cancer. | 2003 Dec 15 |
|
| Effect of combination of TS-1 and low-dose cisplatin on sarcoma-180 mouse sarcoma. | 2003 Jul |
|
| Clinical implications of dihydropyrimidine dehydrogenase (DPD) activity in 5-FU-based chemotherapy: mutations in the DPD gene, and DPD inhibitory fluoropyrimidines. | 2003 Jun |
|
| Phase II trial with S-1 in chemotherapy-naïve patients with gastric cancer. A trial performed by the EORTC Early Clinical Studies Group (ECSG). | 2003 Jun |
|
| Safety and efficacy of S-1, a novel oral fluorouracil antitumor drug, for a chronic renal failure patient maintained on hemodialysis. | 2004 |
|
| Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation. | 2004 Aug 16 |
|
| Bioactivation of capecitabine in human liver: involvement of the cytosolic enzyme on 5'-deoxy-5-fluorocytidine formation. | 2004 Jul |
|
| The effect of food on the pharmacokinetics of S-1 after single oral administration to patients with solid tumors. | 2004 Jun 15 |
|
| Phase II study of S-1 in patients with advanced biliary tract cancer. | 2004 Nov 15 |
|
| Thymidylate synthase predictive power is overcome by irinotecan combination therapy with S-1 for gastric cancer. | 2004 Oct 4 |
|
| 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 Jul |
|
| Correlations between antitumor activities of fluoropyrimidines and DPD activity in lung tumor xenografts. | 2005 Jul |
|
| Phase I trial of oral S-1 combined with gemcitabine in metastatic pancreatic cancer. | 2005 Jun 20 |
|
| Enhancement of the anti-tumor activity of S-1 by low-dose cisplatin in mice bearing the sarcoma-180 model. | 2005 Nov |
|
| [A trial of TS-1 administration on the basis of the pharmacokinetic study for an advanced gastric cancer patient with impaired renal function]. | 2005 Oct |
|
| Randomized scheduling feasibility study of S-1 for adjuvant chemotherapy in advanced head and neck cancer. | 2005 Oct 17 |
|
| The role of thymidylate synthase and dihydropyrimidine dehydrogenase in resistance to 5-fluorouracil in human lung cancer cells. | 2005 Sep |
|
| Phase I/II study of S-1 combined with irinotecan for metastatic advanced gastric cancer. | 2006 Apr 24 |
|
| Potassium oxonate, an enzyme inhibitor compounded in S-1, reduces the suppression of antitumor immunity induced by 5-fluorouracil. | 2006 Aug |
|
| DNA methylation of CHFR is not a predictor of the response to docetaxel and paclitaxel in advanced and recurrent gastric cancer. | 2006 Jan-Feb |
|
| [Combination chemotherapy with S-1 and cisplatin for non-small cell lung cancer]. | 2006 Jun |
|
| Phase II trial of oral S-1 combined with gemcitabine in metastatic pancreatic cancer. | 2006 Jun 5 |
|
| Correlation between the urinary dihydrouracil-uracil ratio and the 5-FU plasma concentration in patients treated with oral 5-FU analogs. | 2006 Sep-Oct |
|
| The significance of the expression of dihydropyrimidine dehydrogenase in prostate cancer. | 2007 Mar |
|
| Phase-I trial of oral fluoropyrimidine anticancer agent (S-1) with concurrent radiotherapy in patients with unresectable pancreatic cancer. | 2007 May 7 |
|
| 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 Oct |
|
| Anti-angiogenic effect of 5-Fluorouracil-based drugs against human colon cancer xenografts. | 2008 Aug 18 |
|
| 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 Aug 19 |
|
| High intratumoral dihydropyrimidine dehydrogenase mRNA levels in pancreatic cancer associated with a high rate of response to S-1. | 2008 Dec |
|
| S-1 monotherapy as a neoadjuvant treatment for locally advanced gastric cancer. | 2008 Mar |
|
| Phase I/II study of oxaliplatin with oral S-1 as first-line therapy for patients with metastatic colorectal cancer. | 2008 Mar 25 |
|
| Combination therapy of S-1 with selective cyclooxygenase-2 inhibitor for liver metastasis of colorectal carcinoma. | 2008 Mar-Apr |
|
| 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 May |
|
| Phase II trial of S-1 and cisplatin with concurrent radiotherapy for locally advanced non-small-cell lung cancer. | 2009 Jul 21 |
|
| N(3)-o-toluyl-fluorouracil inhibits human hepatocellular carcinoma cell growth via sustained release of 5-FU. | 2010 May |
|
| Chemosensitivity test for 5-fluorouracil and 5-chloro-2, 4-dihydroxypyridine predicts outcome of gastric cancer patients receiving S-1 postoperatively. | 2010 Nov |
|
| Gemcitabine and s-1 combination chemotherapy in patients with advanced biliary tract cancer: a retrospective study. | 2010 Sep |
|
| Proteomic differential display analysis for TS-1-resistant and -sensitive pancreatic cancer cells using two-dimensional gel electrophoresis and mass spectrometry. | 2011 Jun |
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.
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
FDA ORPHAN DRUG |
225006
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
||
|
EMA ASSESSMENT REPORTS |
TEYSUNO (AUTHORIZED: STOMACH NEOPLASMS)
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
||
|
NCI_THESAURUS |
C2019
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
C104201
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
C2416
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
DB09257
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
CHEMBL1730601
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
1349387-07-0
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
ALTERNATIVE | |||
|
103766-25-2
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
SUB21055
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
m11875
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
54679224
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
DTXSID8046799
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
7728
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
100000087530
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
1293
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY | |||
|
UA8SE1325T
Created by
admin on Fri Dec 15 16:06:05 GMT 2023 , Edited by admin on Fri Dec 15 16:06:05 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
