Raltitrexed (Tomudex): an alternative choice in patients intolerant to 5-fluorouracil.
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.
Kempin
Sanford
S
Comprehensive Cancer Center, 325 West 15 Street, New York, NY 10011, USA.
Gutierrez
Jorge
J
Wilson
Elizabeth
E
Lowery
Colin
C
Diasio
Robert
R
D000230:Adenocarcinoma / Q000188:drug therapy* / Q000556:secondary; D002288:Adenocarcinoma, Mucinous / Q000188:drug therapy* / Q000556:secondary; D000368:Aged; D000964:Antimetabolites, Antineoplastic / Q000627:therapeutic use*; D003108:Colonic Diseases / Q000188:drug therapy* / Q000473:pathology; D004342:Drug Hypersensitivity / Q000209:etiology*; D005260:Female; D005472:Fluorouracil / Q000009:adverse effects*; D006801:Humans; D002955:Leucovorin / Q000627:therapeutic use; D008207:Lymphatic Metastasis; D008875:Middle Aged; D011799:Quinazolines / Q000627:therapeutic use*; D013876:Thiophenes / Q000627:therapeutic use*; D013940:Thymidylate Synthase / Q000037:antagonists & inhibitors*
D000964:Antimetabolites, Antineoplastic; D011799:Quinazolines; D013876:Thiophenes; D013940:Thymidylate Synthase; C068874:raltitrexed; D002955:Leucovorin; D005472:Fluorouracil