tnp-351 and 2--deoxy-2--methylenecytidine

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.

Topics: Aminopterin; Animals; Antimetabolites, Antineoplastic; Antineoplastic Agents; Cytarabine; Deoxycytidine; Humans; Leukemia L1210; Methotrexate; Mice; Trimetrexate