Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C9H11ClN4O2 |
| Molecular Weight | 242.662 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=C(CN2CCCC2=N)NC(=O)NC1=O
InChI
InChIKey=QQHMKNYGKVVGCZ-UHFFFAOYSA-N
InChI=1S/C9H11ClN4O2/c10-7-5(12-9(16)13-8(7)15)4-14-3-1-2-6(14)11/h11H,1-4H2,(H2,12,13,15,16)
| Molecular Formula | C9H11ClN4O2 |
| Molecular Weight | 242.662 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/28979148 | https://www.ncbi.nlm.nih.gov/pubmed/27568360 | https://www.ncbi.nlm.nih.gov/pubmed/28242161 | https://www.drugbank.ca/drugs/DB09343
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/28979148 | https://www.ncbi.nlm.nih.gov/pubmed/27568360 | https://www.ncbi.nlm.nih.gov/pubmed/28242161 | https://www.drugbank.ca/drugs/DB09343
Tipiracil is a thymidine phosphorylase inhibitor, that used for the treatment of patients with metastatic colorectal cancer. Tipiracil is used in combination with trifluridine as Lonsurf. Trifluridine is incorporated into DNA via phosphorylation, ultimately inhibiting cell proliferation. Tipiracil increases systemic exposure of trifluridine when coadministered. Lonsurf has recently been approved for the treatment of adult patients with metastatic colorectal cancer (mCRC) who are refractory to or are not considered candidates for, current standard chemotherapy and biological therapy in the EU and USA and in unresectable advanced or recurrent CRC in Japan. The approved regimen of oral twice-daily Lonsurf significantly improved overall survival and progression-free survival and was associated with a significantly higher disease control rate than placebo when added to best supportive care in the multinational, pivotal phase III trial (RECOURSE) and a phase II Japanese trial. Trifluridine/tipiracil was associated with an acceptable tolerability profile, with adverse events generally being managed with dose reductions, temporary interruptions in treatment or administration of granulocyte-colony
stimulating factor. The most common grade 3–4 adverse events (>10 %) were anemia, neutropenia, thrombocytopenia, and leukopenia.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3106 |
20.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | LONSURF Approved UseLONSURF is indicated for the treatment of patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. LONSURF is a combination of trifluridine, a nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase inhibitor, indicated for the treatment of patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. (1) Launch Date2015 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
44.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
30 mg/m² 1 times / day multiple, oral dose: 30 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
41.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
40 mg/m² 1 times / day multiple, oral dose: 40 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
50.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
50 mg/m² 1 times / day multiple, oral dose: 50 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
99.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
60 mg/m² 1 times / day multiple, oral dose: 60 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
70 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
70 mg/m² 1 times / day multiple, oral dose: 70 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
234 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
30 mg/m² 1 times / day multiple, oral dose: 30 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
161 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
40 mg/m² 1 times / day multiple, oral dose: 40 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
300 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
50 mg/m² 1 times / day multiple, oral dose: 50 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
447 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
60 mg/m² 1 times / day multiple, oral dose: 60 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
317 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
70 mg/m² 1 times / day multiple, oral dose: 70 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.89 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
30 mg/m² 1 times / day multiple, oral dose: 30 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1.82 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
40 mg/m² 1 times / day multiple, oral dose: 40 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.01 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
50 mg/m² 1 times / day multiple, oral dose: 50 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.21 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
60 mg/m² 1 times / day multiple, oral dose: 60 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.37 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22735906 |
70 mg/m² 1 times / day multiple, oral dose: 70 mg/m² route of administration: Oral experiment type: MULTIPLE co-administered: TRIFLURIDINE |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.4 h |
35 mg/m² 2 times / day steady-state, oral dose: 35 mg/m² route of administration: Oral experiment type: STEADY-STATE co-administered: |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
92% |
35 mg/m² 2 times / day steady-state, oral dose: 35 mg/m² route of administration: Oral experiment type: STEADY-STATE co-administered: |
TIPIRACIL HYDROCHLORIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
50 mg/m2/day 1 times / day multiple, oral MTD Dose: 50 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 50 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
Other AEs: Granulocytopenia, Granulocytopenia... Other AEs: Granulocytopenia (grade 4, 50%) Sources: Granulocytopenia (grade 3, 16.7%) |
100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
DLT: Anemia... Other AEs: Granulocytopenia... Dose limiting toxicities: Anemia (grade 3, 50%) Other AEs:Granulocytopenia (grade 4, 100%) Sources: |
60 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 60 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 60 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
DLT: Granulocytopenia... Other AEs: Granulocytopenia... Dose limiting toxicities: Granulocytopenia (grade 4, 33.3%) Other AEs:Granulocytopenia (grade 3, 33.3%) Sources: |
180 mg/m2/day 1 times / day multiple, oral Highest studied dose|MTD Dose: 180 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 180 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
DLT: Granulocytopenia... Other AEs: Fatigue, Nausea... Dose limiting toxicities: Granulocytopenia (grade 3-4, 66.7%) Other AEs:Fatigue (grade 1-2, 66.7%) Sources: Nausea (grade 1-2, 50%) Diarrhea (grade 1-2, 16.7%) |
110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
DLT: Granulocytopenia... Other AEs: Fatigue, Nausea... Dose limiting toxicities: Granulocytopenia (grade 3-4, 100%) Other AEs:Fatigue (grade 1-2, 66.7%) Sources: Nausea (grade 1-2, 66.7%) Anorexia (grade 1-2, 66.7%) Diarrhea (grade 1-2, 33.3%) Taste abnormality (grade 1-2, 33.3%) Anemia (grade 1-2, 66.7%) Anemia (grade 3-4, 33.3%) |
100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
Other AEs: Fatigue, Anorexia... Other AEs: Fatigue (grade 3-4, 16.7%) Sources: Anorexia (grade 3-4, 16.7%) Granulocytopenia (grade 3-4, 100%) |
120 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 120 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 120 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
DLT: Granulocytopenia... Dose limiting toxicities: Granulocytopenia (grade 3-4, 33.3%) Sources: |
140 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 140 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 140 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
Other AEs: Anemia... Other AEs: Anemia (grade 3-4, 33.3%) Sources: |
150 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 150 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 150 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
Other AEs: Granulocytopenia... Other AEs: Granulocytopenia (grade 3-4, 33.3%) Sources: |
170 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 170 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 170 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
DLT: Nausea, Granulocytopenia... Dose limiting toxicities: Nausea (grade 3, 66.7%) Sources: Granulocytopenia (grade 3-4, 66.7%) |
70 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 70 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 70 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
DLT: Granulocytopenia... Dose limiting toxicities: Granulocytopenia (grade 3-4, 50%) Sources: |
90 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 90 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 90 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
Other AEs: Granulocytopenia, Anemia... Other AEs: Granulocytopenia (grade 3-4, 100%) Sources: Anemia (grade 3-4, 33.3%) |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Neutropenia... AEs leading to discontinuation/dose reduction: Neutropenia (3.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Anemia... AEs leading to discontinuation/dose reduction: Anemia (1.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Febrile neutropenia... AEs leading to discontinuation/dose reduction: Febrile neutropenia (1.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Neutrophil count decreased... AEs leading to discontinuation/dose reduction: Neutrophil count decreased (1.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Fatigue... AEs leading to discontinuation/dose reduction: Fatigue (1.5%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Diarrhea... AEs leading to discontinuation/dose reduction: Diarrhea (1.3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea (0.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Decreased appetite... AEs leading to discontinuation/dose reduction: Decreased appetite (0.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (0.8%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Asthenia... AEs leading to discontinuation/dose reduction: Asthenia (0.6%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Mucosal inflammation... AEs leading to discontinuation/dose reduction: Mucosal inflammation (0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Blood alkaline phosphatase increased... AEs leading to discontinuation/dose reduction: Blood alkaline phosphatase increased (0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Disc. AE: Platelet count decreased... AEs leading to discontinuation/dose reduction: Platelet count decreased (0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Neutropenia... Other AEs: Neutropenia (grade 3-4, 23.8%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Neutrophil count decreased... Other AEs: Neutrophil count decreased (grade 3-4, 18.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Anemia... Other AEs: Anemia (grade 3-4, 15.6%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: White blood cell count decreased... Other AEs: White blood cell count decreased (grade 3-4, 10.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Fatigue... Other AEs: Fatigue (grade 3-4, 3.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Blood bilirubin increased... Other AEs: Blood bilirubin increased (grade 3-4, 3.8%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Febrile neutropenia... Other AEs: Febrile neutropenia (grade 3-4, 3.8%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Decreased appetite... Other AEs: Decreased appetite (grade 3-4, 3.6%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Asthenia... Other AEs: Asthenia (grade 3-4, 3.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Blood alkaline phosphatase increased... Other AEs: Blood alkaline phosphatase increased (grade 3-4, 3.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: GGT increased... Other AEs: GGT increased (grade 3-4, 3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Diarrhea... Other AEs: Diarrhea (grade 3-4, 3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Leukopenia... Other AEs: Leukopenia (grade 3-4, 2.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Platelet count decreased... Other AEs: Platelet count decreased (grade 3-4, 2.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Dyspnea... Other AEs: Dyspnea (grade 3-4, 2.3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: General physical health deterioration... Other AEs: General physical health deterioration (grade 3-4, 2.3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Abdominal pain... Other AEs: Abdominal pain (grade 3-4, 2.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Hypokalemia... Other AEs: Hypokalemia (grade 3-4, 2.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Thrombocytopenia... Other AEs: Thrombocytopenia (grade 3-4, 2.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Vomiting... Other AEs: Vomiting (grade 3-4, 2.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Pyrexia... Other AEs: Pyrexia (grade 3-5, 1.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Constipation... Other AEs: Constipation (grade 3-5, 0.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Cough... Other AEs: Cough (grade 3-5, 0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Edema peripheral... Other AEs: Edema peripheral (grade 3-5, 0.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Stomatitis... Other AEs: Stomatitis (grade 3-5, 0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Back pain... Other AEs: Back pain (grade 3-5, 1.7%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Weight decreased... Other AEs: Weight decreased (grade 3-5, 0.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Abdominal pain upper... Other AEs: Abdominal pain upper (grade 3-5, 0.2%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Ascites... Other AEs: Ascites (grade 3-5, 0.9%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Mucosal inflammation... Other AEs: Mucosal inflammation (grade 3-5, 0.4%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: AST increased... Other AEs: AST increased (grade 3-5, 1.1%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Hyponatremia... Other AEs: Hyponatremia (grade 3-5, 1.3%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Back pain... Other AEs: Back pain (grade 3-5, 1.7%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Tumor pain... Other AEs: Tumor pain (grade 3-5, 0.6%) Sources: |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Other AEs: Hypertension... Other AEs: Hypertension (grade 3-5, 1.5%) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Granulocytopenia | grade 3, 16.7% | 50 mg/m2/day 1 times / day multiple, oral MTD Dose: 50 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 50 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Granulocytopenia | grade 4, 50% | 50 mg/m2/day 1 times / day multiple, oral MTD Dose: 50 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 50 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Anemia | grade 3, 50% DLT |
100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Granulocytopenia | grade 4, 100% | 100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Granulocytopenia | grade 3, 33.3% | 60 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 60 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 60 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Granulocytopenia | grade 4, 33.3% DLT |
60 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 60 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 60 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 54 years Health Status: unhealthy Age Group: median age 54 years Sex: M+F Sources: |
| Diarrhea | grade 1-2, 16.7% | 180 mg/m2/day 1 times / day multiple, oral Highest studied dose|MTD Dose: 180 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 180 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Nausea | grade 1-2, 50% | 180 mg/m2/day 1 times / day multiple, oral Highest studied dose|MTD Dose: 180 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 180 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Fatigue | grade 1-2, 66.7% | 180 mg/m2/day 1 times / day multiple, oral Highest studied dose|MTD Dose: 180 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 180 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 66.7% DLT |
180 mg/m2/day 1 times / day multiple, oral Highest studied dose|MTD Dose: 180 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 180 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Diarrhea | grade 1-2, 33.3% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Taste abnormality | grade 1-2, 33.3% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anemia | grade 1-2, 66.7% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anorexia | grade 1-2, 66.7% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Fatigue | grade 1-2, 66.7% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Nausea | grade 1-2, 66.7% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 100% DLT |
110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anemia | grade 3-4, 33.3% | 110 mg/m2/day 1 times / day multiple, oral MTD Dose: 110 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 110 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 100% | 100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anorexia | grade 3-4, 16.7% | 100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Fatigue | grade 3-4, 16.7% | 100 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 100 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 100 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 33.3% DLT |
120 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 120 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 120 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anemia | grade 3-4, 33.3% | 140 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 140 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 140 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 33.3% | 150 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 150 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 150 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Nausea | grade 3, 66.7% DLT |
170 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 170 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 170 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 66.7% DLT |
170 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 170 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 170 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 50% DLT |
70 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 70 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 70 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Granulocytopenia | grade 3-4, 100% | 90 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 90 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 90 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Anemia | grade 3-4, 33.3% | 90 mg/m2/day 1 times / day multiple, oral Studied dose Dose: 90 mg/m2/day, 1 times / day Route: oral Route: multiple Dose: 90 mg/m2/day, 1 times / day Sources: |
unhealthy, median age 59 years Health Status: unhealthy Age Group: median age 59 years Sex: M+F Sources: |
| Neutropenia | 3.2% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Anemia | 1.9% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Febrile neutropenia | 1.9% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Neutrophil count decreased | 1.9% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Fatigue | 1.5% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Diarrhea | 1.3% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Nausea | 0.9% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Decreased appetite | 0.9% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Vomiting | 0.8% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Asthenia | 0.6% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Mucosal inflammation | 0.4% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Blood alkaline phosphatase increased | 0.4% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Platelet count decreased | 0.4% Disc. AE |
35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Neutropenia | grade 3-4, 23.8% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Neutrophil count decreased | grade 3-4, 18.9% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Anemia | grade 3-4, 15.6% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| White blood cell count decreased | grade 3-4, 10.9% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Fatigue | grade 3-4, 3.9% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Blood bilirubin increased | grade 3-4, 3.8% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Febrile neutropenia | grade 3-4, 3.8% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Decreased appetite | grade 3-4, 3.6% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Asthenia | grade 3-4, 3.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Blood alkaline phosphatase increased | grade 3-4, 3.2% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| GGT increased | grade 3-4, 3% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Diarrhea | grade 3-4, 3% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Leukopenia | grade 3-4, 2.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Platelet count decreased | grade 3-4, 2.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Dyspnea | grade 3-4, 2.3% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| General physical health deterioration | grade 3-4, 2.3% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Abdominal pain | grade 3-4, 2.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Hypokalemia | grade 3-4, 2.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Thrombocytopenia | grade 3-4, 2.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Vomiting | grade 3-4, 2.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Pyrexia | grade 3-5, 1.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Constipation | grade 3-5, 0.2% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Cough | grade 3-5, 0.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Edema peripheral | grade 3-5, 0.2% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Stomatitis | grade 3-5, 0.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Back pain | grade 3-5, 1.7% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Weight decreased | grade 3-5, 0.2% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Abdominal pain upper | grade 3-5, 0.2% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Ascites | grade 3-5, 0.9% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Mucosal inflammation | grade 3-5, 0.4% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| AST increased | grade 3-5, 1.1% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Hyponatremia | grade 3-5, 1.3% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Back pain | grade 3-5, 1.7% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Tumor pain | grade 3-5, 0.6% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
| Hypertension | grade 3-5, 1.5% | 35 mg/m2 2 times / day multiple, oral Recommended Dose: 35 mg/m2, 2 times / day Route: oral Route: multiple Dose: 35 mg/m2, 2 times / day Sources: |
unhealthy, median age 63 years Health Status: unhealthy Age Group: median age 63 years Sex: M+F Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| yes | no (co-administration study) Comment: The population PK analysis suggested that concomitant administration of OCT2 inhibitors (n=24) had no effect on the PK parameters of trifluridine and tipiracil. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207981Orig1s000ClinPharmR.pdf#page=34 Page: 34.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Repeated oral dosing of TAS-102 confers high trifluridine incorporation into DNA and sustained antitumor activity in mouse models. | 2014-12 |
|
| [Influence of the thymidine phosphorylase (platelet-derived endothelial cell growth factor) on tumor angiogenesis. Catalytic activity of enzyme inhibitors]. | 2010 |
|
| Therapeutic potential of the dual-targeted TAS-102 formulation in the treatment of gastrointestinal malignancies. | 2007-06 |
|
| Thymidine phosphorylase from Escherichia coli: tight-binding inhibitors as enzyme active-site titrants. | 2006-02 |
|
| Cooperative stimulation of vascular endothelial growth factor expression by hypoxia and reactive oxygen species: the effect of targeting vascular endothelial growth factor and oxidative stress in an orthotopic xenograft model of bladder carcinoma. | 2005-05-09 |
|
| Pharmacokinetic modeling of species-dependent enhanced bioavailability of trifluorothymidine by thymidine phosphorylase inhibitor. | 2004-06 |
|
| Thymidine kinase and thymidine phosphorylase level as the main predictive parameter for sensitivity to TAS-102 in a mouse model. | 2004-02 |
|
| Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor. | 2004-01 |
|
| Identification of a novel class of inhibitor of human and Escherichia coli thymidine phosphorylase by in silico screening. | 2003-11-03 |
|
| Significance of platelet-derived endothelial cell growth factor in the angiogenesis of human gastric cancer. | 1998-02 |
Patents
Sample Use Guides
In combination with trifluridine, 35 mg/m2 up to a maximum of 80 mg per dose (based on the trifluridine component) orally twice daily within one hour of completion of morning and evening meals on Days 1 through 5 and Days 8 through 12 of each 28-day cycle until disease progression or unacceptable toxicity.
Route of Administration:
Oral
HCT 116, HCT-15, and HT-29 cells were seeded at appropriate concentrations in duplicates in six-well plates. Twenty-four hours after plating, the cells were treated with the trifluridine (FTD 2 mkM or 4 mkM), or IR alone, or the combination of both using the RX-650 CABINET X-Ray system (Faxitron Xray Corp., Wheeling, IL, USA) with 3.4 Gy/min for 0.6-2.4 min. Ten to 12 days after plating, cells were fixed with 20% glutaraldehyde, stained with 0.05% crystal violet, and the number of colonies containing at least 50 cells was determined. Trifluridine enhances the efficacy of IR.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 20:58:18 GMT 2025
by
admin
on
Mon Mar 31 20:58:18 GMT 2025
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| Record UNII |
NGO10K751P
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| Record Status |
Validated (UNII)
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| Record Version |
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Code | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
564116
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NCI_THESAURUS |
C129825
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NDF-RT |
N0000191870
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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NGO10K751P
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PRIMARY | |||
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8696
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PRIMARY | |||
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183204-74-2
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PRIMARY | |||
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CHEMBL235668
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C152646
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PRIMARY | |||
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4893
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PRIMARY | |||
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DB09343
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N0000191869
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PRIMARY | Thymidine Phosphorylase Inhibitors [MoA] | ||
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NGO10K751P
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PRIMARY | |||
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DTXSID601025833
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PRIMARY | |||
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1670304
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PRIMARY | RxNorm | ||
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90879
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PRIMARY | |||
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SUB174128
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PRIMARY | |||
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Tipiracil
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PRIMARY | |||
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6323266
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PRIMARY | |||
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100000160943
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PRIMARY | |||
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9500
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PRIMARY | |||
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BC-15
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PRIMARY | |||
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m11862
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR | |||
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BINDER->LIGAND |
The in vitro protein binding in human plasma is below 8% for tipiracil.
BINDING
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EXCRETED UNCHANGED |
URINE
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| Related Record | Type | Details | ||
|---|---|---|---|---|
|
METABOLITE -> PARENT |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Volume of Distribution | PHARMACOKINETIC |
|
SINGLE DOSE ADMINISTRATION |
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| Biological Half-life | PHARMACOKINETIC |
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SINGLE DOSE ADMINISTRATION |
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