Raltitrexed Tomudex
A drug approved for colorectal cancer. It appears in 10 clinical trials.
What it is
Raltitrexed is a folate analog antimetabolite chemotherapy agent that serves as an alternative to 5-fluorouracil in colorectal cancer treatment. This quinazoline-based cytotoxic drug is primarily used in metastatic colorectal cancer, either as monotherapy or in combination regimens with other agents like S-1 and fruquintinib. Raltitrexed offers a convenient administration schedule compared to continuous infusion 5-FU protocols and has shown efficacy in patients who may not tolerate fluoropyrimidine-based therapies.
How it works
Raltitrexed specifically inhibits thymidylate synthase, a key enzyme in the de novo synthesis of thymidine triphosphate, which is essential for DNA replication and repair. Unlike 5-fluorouracil, raltitrexed is transported into cells via the reduced folate carrier and undergoes polyglutamation, allowing for prolonged intracellular retention and sustained enzyme inhibition. This selective targeting of thymidylate synthase leads to thymidine depletion, DNA strand breaks, and ultimately cancer cell death.
Molecular targets
Common side effects
Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.
Trials with this drug
Guides that may help
Written for patients and families, in plain language.