Folates in current
cancer treatment

The first-line treatment for several types of cancer consists of a combination of chemotherapy and complementary drugs, including folate-based agents aimed at enhancing the effect of chemotherapy. With a new, directly acting folate, the hope is to improve the outlook for those affected by cancer.

Treatment for many forms of cancer is based on a combination of chemotherapy and adjuvant drugs. Current folate-based drugs are metabolized in the body and stepwise converted into the active metabolite [6R]-MTHF. 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 by bypassing the need for conversion. However, such a drug is not yet available on the market.

Arfolitixorin – the next-generation folate drug

Arfolitixorin is being developed as a next-generation folate drug and is direct-acting, which means no conversion is required. Arfolitixorin 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 previous generation folate drugs for a long time.

Arfolitixorin’s potential in other cancer types

Chemotherapy is a central component in the treatment of several types of cancer, and arfolitixorin could hence enhance the efficacy of chemotherapy in multiple patient groups. This opens opportunities to broaden the clinical application of arfolitixorin and thereby potentially increase its commercial value over time.

Drug combinations with 5-FU-based chemotherapy are used not only for colorectal cancer but also for the treatment of pancreatic, gastric, breast, and head and neck cancers, among others. One common trait shared by colorectal cancer and pancreatic cancer is that the cancer cells have a high mutation rate, which means they frequently alter their properties and become difficult to treat and resistant even to modern immunotherapies.

Gastric cancer is a very common form of cancer in Asian populations, but also occurs in Europe, where chemotherapy combined with leucovorin, one of the most common folate drugs, is an established standard in both first-line and later lines of treatment. In lung and breast cancer, treatment strategies also largely target thymidylate synthase (TS), a key enzyme that regulates cell proliferation. This further underscores the potential of arfolitixorin, provided that clinical studies can demonstrate superior efficacy compared to current standard therapies.