Abstract
Raltitrexed (Tomudex), a classical folate antagonist, is a selective inhibitor of thymidylate synthase (TS). It has significant single-agent activity in metastatic colorectal cancer. Severe life-threatening toxicity related to the administration of 5-fluorouracil and leucovorin is described in two patients, both of whom were not deficient in dihydropyrimidine dehydrogenase. Raltitrexed was administered to both patients with clinically acceptable side effects and allowed a TS inhibitor to be administered as part of an adjuvant program.
MeSH terms
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Adenocarcinoma / drug therapy*
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Adenocarcinoma / secondary
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Adenocarcinoma, Mucinous / drug therapy*
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Adenocarcinoma, Mucinous / secondary
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Aged
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Antimetabolites, Antineoplastic / therapeutic use*
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Colonic Diseases / drug therapy*
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Colonic Diseases / pathology
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Drug Hypersensitivity / etiology*
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Female
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Fluorouracil / adverse effects*
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Humans
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Leucovorin / therapeutic use
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Lymphatic Metastasis
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Middle Aged
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Quinazolines / therapeutic use*
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Thiophenes / therapeutic use*
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Thymidylate Synthase / antagonists & inhibitors*
Substances
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Antimetabolites, Antineoplastic
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Quinazolines
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Thiophenes
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Thymidylate Synthase
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raltitrexed
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Leucovorin
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Fluorouracil