raltitrexed

Raltitrexed is a small molecule antimetabolite chemotherapy drug, specifically a quinazoline folate analogue, developed and manufactured by AstraZeneca. It is primarily used for the treatment of advanced colorectal (bowel) cancer, especially in patients who cannot tolerate standard therapies such as capecitabine or fluorouracil-based regimens[1][2][3][7]. Raltitrexed acts as a selective inhibitor of thymidylate synthase, an enzyme essential for DNA synthesis. By mimicking 5,10-methylene tetrahydrofolate and undergoing polyglutamylation within cells, raltitrexed achieves potent and sustained inhibition of thymidylate synthase. This leads to decreased synthesis of thymidine triphosphate (TTP), resulting in DNA fragmentation and cell death[1][5][6]. The drug is administered intravenously every three weeks[2], either alone or in combination with other agents. Raltitrexed has been approved for use in Canada and several European countries since 1998 but is not approved by the US FDA[7]. It may also be considered for other cancers such as malignant mesothelioma.

Brand names

Tomudex

Other names

Thaltitrexed