Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H22N4O6S |
| Molecular Weight | 458.488 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(CC1=CC2=C(C=C1)N=C(C)NC2=O)C3=CC=C(S3)C(=O)N[C@@H](CCC(O)=O)C(O)=O
InChI
InChIKey=IVTVGDXNLFLDRM-HNNXBMFYSA-N
InChI=1S/C21H22N4O6S/c1-11-22-14-4-3-12(9-13(14)19(28)23-11)10-25(2)17-7-6-16(32-17)20(29)24-15(21(30)31)5-8-18(26)27/h3-4,6-7,9,15H,5,8,10H2,1-2H3,(H,24,29)(H,26,27)(H,30,31)(H,22,23,28)/t15-/m0/s1
| Molecular Formula | C21H22N4O6S |
| Molecular Weight | 458.488 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.medicines.org.uk/emc/medicine/2307
https://www.ncbi.nlm.nih.gov/pubmed/21148615
Curator's Comment: Description was created based on several sources, including
https://www.medicines.org.uk/emc/medicine/2307
https://www.ncbi.nlm.nih.gov/pubmed/21148615
Raltitrexed belongs to a group of medicines known as antimetabolites. It is used to treat cancer of the colon and rectum. It may also be used to treat other kinds of cancer, as determined by your doctor. Raltitrexed blocks an enzyme needed by the cell to live. This interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal body cells may also be affected by raltitrexed, other effects will also occur. Some of these may be serious and must be reported to your doctor. Other effects, like hair loss, may not be serious but may cause concern. Raltitrexed inhibits thymidylate synthase (TS) leading to DNA fragmentation and cell death. It is transported into cells via a reduced folate carrier. Inside the cell Raltitrexed is extensively polyglutamated, which enhances thymidylate synthase inhibitory power and duration. Inhibition of this enzyme results in decreased synthesis of thymidine triphosphate which is required for DNA synthesis. Raltitrexed is used for the treatment of malignant neoplasm of colon and rectum. Although raltitrexed is not approved by the US FDA, the drug was licensed in Canada and some European countries.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10550563 | https://www.ncbi.nlm.nih.gov/pubmed/16028105
Curator's Comment: weak penetration
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1952 |
530.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | Tomudex Approved UseThe palliative treatment of advanced colorectal cancer where 5-Fluorouracil and folinic acid based regimens are either not tolerated or inappropriate. Launch Date9.6180483E11 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
567.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9820178 |
3 mg/m² 1 times / day other, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: OTHER co-administered: |
RALTITREXED blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
736.8 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9619761 |
3 mg/m² single, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
RALTITREXED plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1547.9 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9820178 |
3 mg/m² 1 times / day other, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: OTHER co-administered: |
RALTITREXED blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2341.7 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9619761 |
3 mg/m² single, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
RALTITREXED plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.82 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9820178 |
3 mg/m² 1 times / day other, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: OTHER co-administered: |
RALTITREXED blood | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12 min EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/9619761 |
3 mg/m² single, intravenous dose: 3 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
RALTITREXED plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
7% |
RALTITREXED plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
DLT: Asthenia, Granulocytopenia... Other AEs: Leukocytopenia, Nausea... Dose limiting toxicities: Asthenia (grade 3, 33.3%) Other AEs:Granulocytopenia (grade 4, 11.1%) Fatigue (grade 3, 11.1%) Leukocytopenia (grade 3, 11.1%) Sources: Nausea (grade 3, 11.1%) Aspartate aminotransferase increased (grade 3, 11.1%) Alanine aminotransferase increase (grade 3, 33.3%) Bilirubin elevated (grade 3-4, 11.1%) |
3.5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 13 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 13 Sources: |
DLT: Asthenia... Other AEs: Decreased hemoglobin... Dose limiting toxicities: Asthenia (grade 3, 15.4%) Other AEs:Decreased hemoglobin (grade 3, 7.7%) Sources: |
4 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 12 Sources: |
DLT: Granulocytopenia, Bilirubin elevated... Dose limiting toxicities: Granulocytopenia (grade 4, 16.7%) Sources: Bilirubin elevated (grade 4, 8.3%) |
2.5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 2.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 2.5 mg/m2, 1 times / 3 weeks Co-administed with:: 5-iodo-2'-deoxyuridine(10400 mg/m2 IV; every 3 weeks) Sources: |
unhealthy, Median age 62 years n = 3 Health Status: unhealthy Condition: Colorectal Cancer Age Group: Median age 62 years Sex: M+F Population Size: 3 Sources: |
DLT: Neutropenia... Dose limiting toxicities: Neutropenia (grade 4, 66.7%) Sources: |
3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: |
DLT: Leukocytopenia, Transaminases increased... Dose limiting toxicities: Leukocytopenia (grade 3-4, 12.9%) Sources: Transaminases increased (grade 3-4, 10.1%) |
3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
Other AEs: Nausea and vomiting, Diarrhea... Other AEs: Nausea and vomiting (grade 3-4, 11.6%) Sources: Page: 201710/TOMUDEX_PM.pdf - p.9Diarrhea (grade 3-4, 11.1%) Constipation (grade 3-4, 2%) Oral soft tissue conditions (grade 3-4, 2.1%) Pain (grade 3-4, 7.3%) Infection (grade 3-4, 5%) Hemoglobin decreased (grade 3-4, 6.5%) Thrombocytopenia (grade 3-4, 3.5%) Blood bilirubin decreased (grade 3-4, 2.2%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Aspartate aminotransferase increased | grade 3, 11.1% | 4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Leukocytopenia | grade 3, 11.1% | 4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Nausea | grade 3, 11.1% | 4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Fatigue | grade 3, 11.1% DLT |
4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Alanine aminotransferase increase | grade 3, 33.3% | 4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Asthenia | grade 3, 33.3% DLT |
4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Bilirubin elevated | grade 3-4, 11.1% | 4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Granulocytopenia | grade 4, 11.1% DLT |
4.5 mg/m2 1 times / 3 weeks multiple, intravenous Highest studied dose|MTD Dose: 4.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 9 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 9 Sources: |
| Asthenia | grade 3, 15.4% DLT |
3.5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 13 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 13 Sources: |
| Decreased hemoglobin | grade 3, 7.7% | 3.5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3.5 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 13 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 13 Sources: |
| Granulocytopenia | grade 4, 16.7% DLT |
4 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 12 Sources: |
| Bilirubin elevated | grade 4, 8.3% DLT |
4 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 4 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 4 mg/m2, 1 times / 3 weeks Sources: |
unhealthy, Median age 55.5 years n = 12 Health Status: unhealthy Condition: solid tumors Age Group: Median age 55.5 years Sex: M+F Population Size: 12 Sources: |
| Neutropenia | grade 4, 66.7% DLT |
2.5 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 2.5 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 2.5 mg/m2, 1 times / 3 weeks Co-administed with:: 5-iodo-2'-deoxyuridine(10400 mg/m2 IV; every 3 weeks) Sources: |
unhealthy, Median age 62 years n = 3 Health Status: unhealthy Condition: Colorectal Cancer Age Group: Median age 62 years Sex: M+F Population Size: 3 Sources: |
| Transaminases increased | grade 3-4, 10.1% DLT |
3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: |
| Leukocytopenia | grade 3-4, 12.9% DLT |
3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: |
| Diarrhea | grade 3-4, 11.1% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Nausea and vomiting | grade 3-4, 11.6% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Constipation | grade 3-4, 2% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Oral soft tissue conditions | grade 3-4, 2.1% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Blood bilirubin decreased | grade 3-4, 2.2% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Thrombocytopenia | grade 3-4, 3.5% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Infection | grade 3-4, 5% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Hemoglobin decreased | grade 3-4, 6.5% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
| Pain | grade 3-4, 7.3% | 3 mg/m2 1 times / 3 weeks multiple, intravenous Studied dose Dose: 3 mg/m2, 1 times / 3 weeks Route: intravenous Route: multiple Dose: 3 mg/m2, 1 times / 3 weeks Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
unhealthy n = 861 Health Status: unhealthy Condition: Colorectal Cancer Sex: M+F Population Size: 861 Sources: Page: 201710/TOMUDEX_PM.pdf - p.9 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no [IC50 133 uM] | ||||
| no [IC50 133 uM] | ||||
| no [IC50 133 uM] | ||||
| no [IC50 133 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes [Km 43.7 uM] | ||||
| yes |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Characterization and drug sensitivity of four newly established colon adenocarcinoma cell lines to antifolate inhibitors of thymidylate synthase. | 2001 |
|
| A phase I study of raltitrexed (Tomudex) combined with carmofur in metastatic colorectal cancer. | 2001 |
|
| Molecular and cellular biology of the human reduced folate carrier. | 2001 |
|
| Management of chemotherapy-induced adverse effects in the treatment of colorectal cancer. | 2001 |
|
| The role of irinotecan and oxaliplatin in the treatment of advanced colorectal cancer. | 2001 Apr |
|
| [Oxaliplatin in combination with non fluoropyrimidine drugs in colorectal cancer]. | 2001 Aug |
|
| [Assessment of the cost of first line chemotherapy in metastatic colorectal cancer. Preliminary results in the FFCD 9601 trial]. | 2001 Aug-Sep |
|
| Metastatic colorectal cancer. | 2001 Dec |
|
| [Raltitrexed in colorectal cancer]. | 2001 Jan-Feb |
|
| The impact of p53 status on cellular sensitivity to antifolate drugs. | 2001 Jul |
|
| New therapies, new directions: advances in the systemic treatment of metastatic colorectal cancer. | 2001 May |
|
| Phase I trial of sequential administration of raltitrexed (Tomudex) and 5-iodo-2'-deoxyuridine (IdUrd). | 2001 May |
|
| Combined effects of adenovirus-mediated wild-type p53 transduction, temozolomide and poly (ADP-ribose) polymerase inhibitor in mismatch repair deficient and non-proliferating tumor cells. | 2001 May |
|
| Crystal structure of a deletion mutant of human thymidylate synthase Delta (7-29) and its ternary complex with Tomudex and dUMP. | 2001 May |
|
| Modulation of both endogenous folates and thymidine enhance the therapeutic efficacy of thymidylate synthase inhibitors. | 2001 May 1 |
|
| Single nucleotide polymorphisms in the human reduced folate carrier: characterization of a high-frequency G/A variant at position 80 and transport properties of the His(27) and Arg(27) carriers. | 2001 Nov |
|
| Preoperative chemoradiation with raltitrexed ('Tomudex') for T2/N+ and T3/N+ rectal cancers: a phase I study. | 2001 Nov |
|
| [Colorectal cancer: irinotecan in combination with newer drugs]. | 2001 Nov-Dec |
|
| Oxaliplatin and raltitrexed in the treatment of inoperable malignant pleural mesothelioma: results of a pilot study. | 2001 Nov-Dec |
|
| Phase I clinical and pharmacogenetic trial of irinotecan and raltitrexed administered every 21 days to patients with cancer. | 2001 Oct 15 |
|
| Multicenter phase II trial of dose-fractionated irinotecan in patients with advanced colorectal cancer failing oxaliplatin-based first-line combination chemotherapy. | 2001 Sep |
|
| [Recent aspects of palliative treatment of metastasized colorectal carcinoma]. | 2001 Sep 15 |
|
| [Raltitrexed and oxaliplatin in colorectal cancer: in vitro and in vivo study of a synergistic cytostatic combination]. | 2002 |
|
| Chemotherapy in colorectal cancer: new options and new challenges. | 2002 |
|
| Cisplatin, raltitrexed, levofolinic acid and 5-fluorouracil in locally advanced or metastatic squamous cell carcinoma of the head and neck: a phase II randomized study. | 2002 |
|
| Multicenter phase I study of irinotecan plus raltitrexed in patients with 5-fluorouracil-refractory advanced colorectal cancer. | 2002 |
|
| Raltitrexed: current clinical status and future directions. | 2002 Apr |
|
| Pemetrexed for diffuse malignant pleural mesothelioma. | 2002 Apr |
|
| Raltitrexed plus oxaliplatin as first-line chemotherapy in metastatic colorectal carcinoma: a multicentric phase II trial. | 2002 Aug |
|
| The means to an end of tumor cell resistance to chemotherapeutic drugs targeting thymidylate synthase: shoot the messenger. | 2002 Aug |
|
| Effects of antifolates on the binding of 5-fluoro-2'-deoxyuridine monophosphate to thymidylate synthase. | 2002 Aug 15 |
|
| Raltitrexed (tomudex) administration in patients failing multiple prior chemotherapy regimens in advanced colorectal cancer: a pilot study. | 2002 Feb |
|
| The emerging role of antifolates in the treatment of malignant pleural mesothelioma. | 2002 Feb |
|
| Clinical and immunological assessment of Mycobacterium vaccae (SRL172) with chemotherapy in patients with malignant mesothelioma. | 2002 Feb 1 |
|
| Nucleoside transport inhibitors, dipyridamole and p-nitrobenzylthioinosine, selectively potentiate the antitumor activity of NB1011. | 2002 Jan |
|
| Randomized multicenter phase II trial of oxaliplatin plus irinotecan versus raltitrexed as first-line treatment in advanced colorectal cancer. | 2002 Jan 1 |
|
| Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis. | 2002 Jan 15 |
|
| [The new chemotherapy of colorectal cancers]. | 2002 Jan 26 |
|
| Multicenter non-randomized phase II study of raltitrexed (Tomudex) and oxaliplatin in non-pretreated metastatic colorectal cancer patients. | 2002 Jul |
|
| Advanced colorectal cancer treatment in Europe: what have we achieved? | 2002 Jun |
|
| Raltitrexed in the treatment of elderly patients with advanced colorectal cancer: an active and low toxicity regimen. | 2002 Jun |
|
| Oxaliplatin plus raltitrexed and leucovorin-modulated 5-fluorouracil i.v. bolus: a salvage regimen for colorectal cancer patients. | 2002 Jun 17 |
|
| Costs and consequences of different chemotherapy regimens in metastatic colorectal cancer. | 2002 Jun 5 |
|
| Efficacy, tolerability and management of raltitrexed (Tomudex) monotherapy in patients with advanced colorectal cancer. a review of phase II/III trials. | 2002 Mar |
|
| Combined chemotherapy trials require combined pharmacogenetic approaches. | 2002 Mar 1 |
|
| Sequence-dependent effects of ZD1839 ('Iressa') in combination with cytotoxic treatment in human head and neck cancer. | 2002 Mar 4 |
|
| Oxaliplatin: results in colorectal carcinoma. | 2002 Oct |
|
| Ex vivo stimulation of renal transport of the cytostatic drugs methotrexate, cisplatin, topotecan (Hycamtin) and raltitrexed (Tomudex) by dexamethasone, T3 and EGF in intact human and rat kidney tissue and in human renal cell carcinoma. | 2002 Sep |
|
| Irinotecan and raltitrexed: an active combination in advanced colorectal cancer. | 2002 Sep |
|
| Raltitrexed treatment promotes systemic inflammatory reaction in patients with colorectal carcinoma. | 2002 Sep 9 |
Sample Use Guides
The recommended dose is 3 mg/m2 given intravenously, as a single short, intravenous infusion in 50 to 250 ml of either 0.9% sodium chloride solution or 5% dextrose (glucose) solution. It is recommended that the infusion is given over a 15 minute period. Other drugs should not be mixed with 'Tomudex' (raltitrexed) in the same infusion container. In the absence of toxicity, treatment may be repeated every 3 weeks.
Dose escalation above 3 mg/m2 is not recommended, since higher doses have been associated with an increased incidence of life-threatening or fatal toxicity.
Route of Administration:
Intravenous
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:32:14 UTC 2023
by
admin
on
Fri Dec 15 15:32:14 UTC 2023
|
| Record UNII |
FCB9EGG971
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
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Official Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Brand Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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NCI_THESAURUS |
C511
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
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WHO-VATC |
QL01BA03
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
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WHO-ATC |
L01BA03
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
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|
NCI_THESAURUS |
C2021
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
DTXSID0046482
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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2353
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
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PRIMARY | |||
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SUB10244MIG
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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FCB9EGG971
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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7403
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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m9487
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | Merck Index | ||
|
RALTITREXED
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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C068874
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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CHEMBL225071
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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112887-68-0
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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135400182
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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7319
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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100000080291
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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196239
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | RxNorm | ||
|
II-28
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
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DB00293
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY | |||
|
C1804
Created by
admin on Fri Dec 15 15:32:15 UTC 2023 , Edited by admin on Fri Dec 15 15:32:15 UTC 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TRANSPORTER -> SUBSTRATE |
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SALT/SOLVATE -> PARENT |
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|
TARGET -> INHIBITOR |
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
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