Research Area: Cancer
Biological Activity:
Raltitrexed (Tomudex) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. Raltitrexed (Tomudex) is an antimetabolite drug used in cancer chemotherapy. Raltitrexed (Tomudex) is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting Dihydrofolate reductase, an enzyme used in the synthesis of tetrahydrofolate, thereby preventing the synthesis of thymidylate. [1] In a study, there was an inverse relationship between reduced folate cellular content and raltitrexed IC50; this relationship did not, however, reach statistical significance. The only significant relationship was found between basal cellular folylpolyglutamate synthetase activity and raltitrexed IC50r = -0.56, p = 0.03. Tumor cells with a relatively high folylpolyglutamate synthetase activity were more sensitive to raltitrexed cytotoxic effects and vice versa.[2]References on Raltitrexed (Tomudex)[1] http://en.wikipedia.org/wiki/Raltitrexed, , [2] http://www.medscape.com/viewarticle/456039_4, , |