ARFOLITIXORIN CONTAINS THE KEY ACTIVE METABOLITE OF ALL CLINICALLY USED FOLATE-BASED DRUGS
arfolitixorin is Isofol’s clinical lead candidate, a novel folate-based therapy developed to increase the efficacy and reduce the side effects of antimetabolites used in cancer treatment. The active pharmaceutical ingredient (API) of arfolitixorin is the key active metabolite of all clinically used folate-based drugs today, including leucovorin and levoleucovorin, and does therefore not require metabolic activation to exert its action. As part of their cancer treatments, more than 500 000 patients are treated with folate-based therapies annually, in the US, Europe and Japan – more than any other single cancer drug.
A MAJORITY OF PATIENTS DO NOT FULLY BENEFIT FROM THEIR FOLATE-BASED THERAPIES TODAY
All current folate-based therapies used in cancer treatment are prodrugs that need multiple activation steps into an active metabolite to exert their actions. Isofol has shown that a few genes determine cancer patients’ ability to activate these prodrugs. By purifying the key active metabolite of all the marketed folate-based prodrugs, Isofol has created a product that does not require metabolic activation to exert its action. Against this background, arfolitixorin may be beneficial regardless of the patient’s genetic ability to activate folates and thus holds the potential to replace the folates used in cancer treatment today.
MULTIPLE METABOLIC STEPS REQUIRED TO CONVERT LEUCOVORIN
ARFOLITIXORIN INCLUDES THE ACTIVE METABOLITE OF ALL FOLATE-BASED THERAPIES
ARFOLITIXORIN – INNOVATION THROUGH COLLABORATION
It was not until 2005 that the active ingredient of arfolitixorin could be commercially manufactured when Merck & Cie developed and patented a production method. Isofol collaborates closely with Merck & Cie, who are the world’s leading manufacturer of reduced folates. Isofol has a worldwide, exclusive and sub-licensable supply and license agreement for arfolitixorin in oncology. The GMP production process for arfolitixorin is patent protected and has been validated. Recipharm produced the first large-scale technical GMP batch for Isofol in October, 2016.
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