title: [Development of antimetabolites, II].
abstract: Two analogues of cytosine arabinoside (ara-C) and three analogues of methotrexate (MTX) are under their clinical studies in Japan. Gemcitabine and DMDC are analogues of ara-C, showing similar antitumor efficacies each other and rather mild animal toxicities. Currently, dFdC is under phase II study, showing activity against lung cancer and DMDC under phase I study. As for MTX analogues, edatrexate, trimetrexate and TNP-351 have been put on the clinical phase studies. Among these antifolates, both edatrexate and trimetrexate have showed responses against lung cancer and we expect that TNP-351 may also show a similar response in the future. Currently, phase II studies of edatrexate and trimetrexate and phase I study of TNP-351 are under progress.
authors.affiliation: Cancer Chemotherapy Center, Japanese Foundation for Cancer Research.
authors.forename: S
authors.initials: S
authors.lastname: Tsukagoshi
mesh_terms: D000630:Aminopterin / Q000031:analogs & derivatives / Q000627:therapeutic use; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000627:therapeutic use; D003561:Cytarabine / Q000031:analogs & derivatives / Q000627:therapeutic use; D003841:Deoxycytidine / Q000031:analogs & derivatives / Q000627:therapeutic use; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D008727:Methotrexate / Q000031:analogs & derivatives / Q000627:therapeutic use; D051379:Mice; D016597:Trimetrexate / Q000627:therapeutic use
chemical_list: D000964:Antimetabolites, Antineoplastic; D000970:Antineoplastic Agents; D003561:Cytarabine; D003841:Deoxycytidine; C078101:TNP 351; C056034:2'-deoxy-2'-methylenecytidine; C040210:edatrexate; D000630:Aminopterin; D016597:Trimetrexate; D008727:Methotrexate