Raltitrexed

General information

Raltitrexed is a specific inhibitor of thymidylate synthase. It is used to treat colorectal cancers.

In about 1000 patients with advanced colorectal cancer, the dose-limiting toxic effects in phase 1 studies were gastrointestinal toxicity, myelosuppression, and weakness; adverse events during phase 2 and 3 studies were similar to those seen during phase 1 [ ]. In all comparative studies, mucositis and leukopenia were markedly less common and less severe in patients treated with raltitrexed than with bolus fluorouracil + leucovorin. Thrombocytopenia was more common with raltitrexed but it was not associated with an increase in clinically significant hemorrhage. In contrast, raltitrexed-related myelosuppression was more severe than with fluorouracil + leucovorin when the anti-metabolite was given by continuous infusion. Raised aminotransferase activities were common with raltitrexed but were usually reversible with continued dosing and were not associated with clinical sequelae.

Organs and systems