Merck Eprova and Isofol Medical Enter Exclusive Agreement for Merck Eprova's Modufolin in oncology

12-Nov-2009 - Switzerland

Merck Eprova AG announced that the company has signed an exclusive license agreement with Isofol Medical AB of Sweden to utilize Merck Eprova’s proprietary folate compound Modufolin® in oncology. The use of Modufolin® is expected to enhance effectiveness compared to currently used folate compounds in cancer treatment. Merck Eprova AG will be providing Modufolin®, the active metabolite of LV (Leucovorin), for use in clinical trials and commercial drug products.

After years of intensive research, Merck Eprova AG has succeeded in developing a stable form of the reduced folate Modufolin® ([6R]-5,10-methylenetetrahydrofolate). This breakthrough opens an avenue for testing novel folate-based drug combinations in cancer treatment.

Modufolin® is a biomodulator originally designed to replace LV as the preferred folate to enhance the activity and reduce associated toxicity of 5-FU (5-fluorouracil), a widely used anti-cancer drug. The active form of 5-FU is an inhibitor of the key enzyme TS (thymidylate synthase). Blocking the synthesis of the nucleotide thymidine leads to inhibition of DNA replication and cell death. The effectiveness of 5-FU/LV in combination therapy may be limited due to several metabolic conversions of LV required to generate the pharmacologically active folate compound Modufolin®. In contrast Modufolin® does not need any further metabolic activation. In the tumour tissue this specific form of folate is directly usable by the target enzyme TS, potentially allowing 5-FU to work more effectively.

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