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Raltitrexed is a three-weekly intravenous antifolate used in Europe, Canada and Australia for advanced bowel cancer, and with cisplatin for mesothelioma, in patients who cannot take fluorouracil.
Raltitrexed (Tomudex) was developed by ICI and Zeneca as a direct thymidylate synthase inhibitor that does not need the metabolic activation fluorouracil needs. It is approved in the United Kingdom, much of Europe, Canada and Australia for palliative treatment of advanced colorectal cancer and, in several countries, with cisplatin for malignant pleural mesothelioma on the strength of a European phase 3 trial. It was never approved in the United States after early deaths in a comparative trial. Its main use today is as a fluorouracil substitute in patients with cardiac toxicity from fluoropyrimidines.
A quinazoline antifolate taken up by the reduced folate carrier and polyglutamated inside cells, where it inhibits thymidylate synthase directly and so starves DNA synthesis of thymidine. Connects to Thymidylate synthase (TYMS).
1.Raltitrexed slips into a pocket on Thymidylate synthase (TYMS).
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Query for this drug: (TITLE:"Raltitrexed" OR ABSTRACT:"Raltitrexed" OR TITLE:"Tomudex" OR ABSTRACT:"Tomudex" OR TITLE:"ZD1694" OR ABSTRACT:"ZD1694") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Raltitrexed, not a curated reading list.
Shares Thymidylate synthase (TYMS), Fluorouracil (5-FU), Cytotoxic chemotherapy, Colorectal cancer and the tag chembl-universe.
Shares Thymidylate synthase (TYMS), Fluorouracil (5-FU), Cytotoxic chemotherapy, Colorectal cancer and the tag chembl-universe.
Shares Fluorouracil (5-FU), Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.