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 Date2000 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Sources: |
unhealthy, Median age 62 years Health Status: unhealthy Age Group: Median age 62 years Sex: M+F 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 Health Status: unhealthy Sex: M+F 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Other AEs: Nausea and vomiting, Diarrhea... Other AEs: Nausea and vomiting (grade 3-4, 11.6%) Sources: Diarrhea (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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Health Status: unhealthy Age Group: Median age 55.5 years Sex: M+F 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 Sources: |
unhealthy, Median age 62 years Health Status: unhealthy Age Group: Median age 62 years Sex: M+F 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 Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
| 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: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
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 |
|---|---|---|
| Oxaliplatin: results in colorectal carcinoma. | 2002-10 |
|
| Phase I and pharmacokinetic study of irinotecan in combination with raltitrexed. | 2002-10 |
|
| Raltitrexed treatment promotes systemic inflammatory reaction in patients with colorectal carcinoma. | 2002-09-09 |
|
| 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. | 2002-09 |
|
| Irinotecan and raltitrexed: an active combination in advanced colorectal cancer. | 2002-09 |
|
| Effects of antifolates on the binding of 5-fluoro-2'-deoxyuridine monophosphate to thymidylate synthase. | 2002-08-15 |
|
| Second-Line Treatment of Advanced Colorectal Cancer with a Biweekly Oxaliplatin plus Irinotecan Combination Regimen. | 2002-08 |
|
| Raltitrexed plus oxaliplatin as first-line chemotherapy in metastatic colorectal carcinoma: a multicentric phase II trial. | 2002-08 |
|
| The means to an end of tumor cell resistance to chemotherapeutic drugs targeting thymidylate synthase: shoot the messenger. | 2002-08 |
|
| A rationale for the clinical development of the thymidylate synthase inhibitor ZD9331 in ovarian and other solid tumours. | 2002-07-18 |
|
| Multicenter non-randomized phase II study of raltitrexed (Tomudex) and oxaliplatin in non-pretreated metastatic colorectal cancer patients. | 2002-07 |
|
| Baseline quality of life predicts survival in patients with advanced colorectal cancer. | 2002-07 |
|
| Oxaliplatin plus raltitrexed and leucovorin-modulated 5-fluorouracil i.v. bolus: a salvage regimen for colorectal cancer patients. | 2002-06-17 |
|
| Costs and consequences of different chemotherapy regimens in metastatic colorectal cancer. | 2002-06-05 |
|
| Which endpoints should we use in evaluating the use of novel fluoropyrimidine regimens in colorectal cancer? | 2002-06-05 |
|
| Why hasn't the National Institute been 'NICE' to patients with colorectal cancer? National Institute of Clinical Excellence. | 2002-06-05 |
|
| Ralitrexed (Tomudex) or Nordic-FLv regimen in metastatic colorectal cancer: a randomized phase II study focusing on quality of life, patients' preferences and health economics. | 2002-06 |
|
| Advanced colorectal cancer treatment in Europe: what have we achieved? | 2002-06 |
|
| Raltitrexed in the treatment of elderly patients with advanced colorectal cancer: an active and low toxicity regimen. | 2002-06 |
|
| [Colorectal cancer: irinotecan in combination with newer drugs]. | 2002-05-09 |
|
| [Oxaliplatin: combinations with thymidylate synthetase inhibitors: two consecutive phase II studies]. | 2002-05-09 |
|
| Oxaliplatin and raltitrexed in the treatment of inoperable malignant pleural mesothelioma: results of a pilot study. | 2002-05-07 |
|
| Comparison of survival, palliation, and quality of life with three chemotherapy regimens in metastatic colorectal cancer: a multicentre randomised trial. | 2002-05-04 |
|
| Raltitrexed plus oxaliplatin (TOMOX) as first-line chemotherapy for metastatic colorectal cancer. A phase II study of the Italian Group for the Study of Gastrointestinal Tract Carcinomas (GISCAD). | 2002-05 |
|
| Phase I dose-escalating study of raltitrexed ('Tomudex') and cisplatin in metastatic non-small cell lung cancer. | 2002-05 |
|
| [Intraoperative radiotherapy (IORT) in the treatment of rectal cancer]. | 2002-04-27 |
|
| Present indications for adjuvant therapy in resectable rectal cancer. | 2002-04-27 |
|
| Raltitrexed: current clinical status and future directions. | 2002-04 |
|
| Pemetrexed for diffuse malignant pleural mesothelioma. | 2002-04 |
|
| Sequence-dependent effects of ZD1839 ('Iressa') in combination with cytotoxic treatment in human head and neck cancer. | 2002-03-04 |
|
| Combined chemotherapy trials require combined pharmacogenetic approaches. | 2002-03-01 |
|
| Update on pharmacogenetics in cancer chemotherapy. | 2002-03 |
|
| Efficacy, tolerability and management of raltitrexed (Tomudex) monotherapy in patients with advanced colorectal cancer. a review of phase II/III trials. | 2002-03 |
|
| Clinical and immunological assessment of Mycobacterium vaccae (SRL172) with chemotherapy in patients with malignant mesothelioma. | 2002-02-01 |
|
| Raltitrexed (tomudex) administration in patients failing multiple prior chemotherapy regimens in advanced colorectal cancer: a pilot study. | 2002-02 |
|
| The emerging role of antifolates in the treatment of malignant pleural mesothelioma. | 2002-02 |
|
| [The new chemotherapy of colorectal cancers]. | 2002-01-26 |
|
| Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis. | 2002-01-15 |
|
| Nucleoside transport inhibitors, dipyridamole and p-nitrobenzylthioinosine, selectively potentiate the antitumor activity of NB1011. | 2002-01 |
|
| [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 |
|
| [The rare manifestation of soft tissue metastasis in colorectal cancer]. | 2002 |
|
| Conjoint analysis of a new Chemotherapy: willingness to pay and preference for the features of raltitrexed versus standard therapy in advanced Colorectal Cancer. | 2002 |
|
| Raltitrexed as monochemotherapy induces a statistically significant increase in platelet count. | 2002 |
|
| Multicenter phase I study of irinotecan plus raltitrexed in patients with 5-fluorouracil-refractory advanced colorectal cancer. | 2002 |
|
| Raltitrexed (Tomudex) administration in patients with relapsed metastatic colorectal cancer after weekly irinotecan/5-Fluorouracil/Leucovorin chemotherapy. | 2002 |
|
| Metastatic colorectal cancer. | 2001-12 |
|
| New therapies, new directions: advances in the systemic treatment of metastatic colorectal cancer. | 2001-05 |
|
| A rapid and systematic review of the evidence for the clinical effectiveness and cost-effectiveness of irinotecan, oxaliplatin and raltitrexed for the treatment of advanced colorectal cancer. | 2001 |
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
Mon Mar 31 18:00:25 GMT 2025
by
admin
on
Mon Mar 31 18:00:25 GMT 2025
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| Record UNII |
FCB9EGG971
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| Record Status |
Validated (UNII)
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NCI_THESAURUS |
C511
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WHO-VATC |
QL01BA03
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WHO-ATC |
L01BA03
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NCI_THESAURUS |
C2021
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DTXSID0046482
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2353
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SUB10244MIG
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FCB9EGG971
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7403
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m9487
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RALTITREXED
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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C068874
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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CHEMBL225071
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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112887-68-0
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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135400182
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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7319
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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100000080291
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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196239
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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II-28
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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DB00293
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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C1804
Created by
admin on Mon Mar 31 18:00:25 GMT 2025 , Edited by admin on Mon Mar 31 18:00:25 GMT 2025
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| Related Record | Type | Details | ||
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TRANSPORTER -> SUBSTRATE |
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
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