Raltitrexed

Raltitrexed (Tomudex) is a chemotherapy drug used for the treatment of colorectal cancer, and other types of cancer. It is a thymidylate synthase inhibitor that prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.

Mechanism of Action

Raltitrexed is a quinazoline derivative that acts as an inhibitor of the enzyme thymidylate synthase. This enzyme is necessary for the synthesis of thymidine, one of the building blocks of DNA and RNA. By inhibiting this enzyme, Raltitrexed prevents the formation of these essential molecules, thereby stopping the growth and proliferation of cancer cells.

Clinical Use

Raltitrexed is primarily used in the treatment of advanced colorectal cancer. It is often used when other treatments, such as 5-fluorouracil (5-FU), are not suitable or have failed. It may also be used in the treatment of other types of cancer, such as mesothelioma and stomach cancer, although its use in these cases is less common.

Side Effects

Like all chemotherapy drugs, Raltitrexed can cause side effects. These may include nausea, vomiting, diarrhea, stomatitis (inflammation of the mouth), and leukopenia (a decrease in white blood cells). More serious side effects can include neutropenia (a severe decrease in white blood cells), which can increase the risk of infection, and thrombocytopenia (a decrease in platelets), which can increase the risk of bleeding.

Pharmacokinetics

Raltitrexed is administered intravenously. It is extensively metabolized in the liver, and its metabolites are primarily excreted in the urine. The half-life of Raltitrexed is approximately 10 hours.

See Also

• Chemotherapy
• Colorectal cancer
• Thymidylate synthase