Drug intelligence / Profile preview

dichloromethotrexate

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Small Molecules
01

Overview

Dichloromethotrexate is a chemical derivative of methotrexate in which two chlorine atoms are substituted at the 3' and 5' positions on the benzoyl ring. Like methotrexate, it is an antimetabolite and antifolate agent. Its mechanism of action is expected to be similar to that of methotrexate—competitive inhibition of dihydrofolate reductase (DHFR), leading to impaired synthesis of DNA and RNA due to reduced availability of tetrahydrofolates required for nucleotide synthesis[10][7]. This results in suppression of rapidly dividing cells such as cancer cells. Dichloromethotrexate has been studied primarily as an experimental anticancer agent but has not achieved widespread clinical use or approval.

Other names
3',5'-dichloromethotrexatemethotrexate dichloro-amethopterin,5'-dichloro-glutamic acid,5-dichloro-4-([(2,4-diamino-6-pteridinyl)methyl]methylamino)benzoyl)-[8]
02

Targets

DHFR (Dihydrofolate reductase)

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