[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: S Tsukagoshi
• Journal: Gan to kagaku ryoho. Cancer & chemotherapy (Gan To Kagaku Ryoho) Vol. 20 Issue 1 Pg. 19-26 (Jan 1993) ISSN: 0385-0684 [Print] Japan
• PMID: 8422184 (Publication Type: Journal Article, Review)

Chemical References

• Antimetabolites, Antineoplastic
• Antineoplastic Agents
• Cytarabine
• Deoxycytidine
• TNP 351
• 2'-deoxy-2'-methylenecytidine
• edatrexate
• Aminopterin
• Trimetrexate
• Methotrexate

Topics

• Aminopterin (analogs & derivatives, therapeutic use)
• Animals
• Antimetabolites, Antineoplastic (therapeutic use)
• Antineoplastic Agents (therapeutic use)
• Cytarabine (analogs & derivatives, therapeutic use)
• Deoxycytidine (analogs & derivatives, therapeutic use)
• Humans
• Leukemia L1210 (drug therapy)
• Methotrexate (analogs & derivatives, therapeutic use)
• Mice
• Trimetrexate (therapeutic use)