Folates in current
cancer treatment

Treatment for many forms of cancer is based on a combination of chemotherapy and adjuvant drugs. Folate-based drugs are sometimes used to enhance the efficacy of certain chemotherapy. These are metabolized in the body and progressively converted into the active metabolite [6R]-MTHF, which both enhances the cytotoxic effects of chemotherapy against tumor cells and inhibits the synthesis of essential building blocks required for tumor growth.

Since the conversion of current folate-based drugs to the active metabolite occurs through multiple steps, treatment with a direct-acting metabolite can probably offer significant clinical advantages. However, such a drug is not yet available on the market.

Arfolitixorin is being developed as a next-generation folate drug and is direct-acting, which means no conversion is required. Arfoltixorin is designed to deliver substantially higher concentrations of the active metabolite to tumor cells than existing drugs. This could potentially result in more effective cancer treatment and thereby benefit a greater number of patients.

For several cancer types, folate-based drugs are already established in first-line treatment – the standardized initial treatment for a disease. For example, chemotherapy based on 5-FU, which is used in the treatment of colorectal cancer and other gastrointestinal cancers, has been combined with folate drugs for a long time. If arfolitixorin demonstrates favorable efficacy in clinical trials, the drug candidate therefore has a unique opportunity to enhance the effectiveness of standard of care for several aggressive forms of cancer.