Diatos obtained exclusive, worldwide rights to DTS-108, a prodrug of irinotecan.



Diatos has granted Drais Pharmaceuticals rights to DTS-108, an early-stage pro-drug to treat solid tumors. This exclusive, worldwide agreement is worth $46.9 million plus royalties.


DTS-108 is ready to begin Phase I trials in Europe for the treatment of patients with advanced or metastatic solid tumors, according to the companies. Drais may develop and commercialize the compound worldwide. In return, Diatos will receive an upfront payment, development and sales milestones, as well as royalties.


DTS-108 is a pro-drug of SN38, the active metabolite of irinotecan, a chemotherapy agent. Irinotecan is an antineoplastic enzyme inhibitor of the topoisomerase I inhibitor class primarily used in the treatment of colorectal cancer. Irinotecan is a derivative of camptothecin, which interacts specifically with the enzyme topoisomerase I to relieve torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks, the firms explain.


Current research suggests that the cytotoxicity of irinotecan is due to double-strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topoisomerase I, DNA, and either irinotecan or SN-38, according to the partners. By applying its Vectocell technology, Diatos has shown in nonclinical models that it can deliver high doses of SN38, while avoiding the gastrointestinal toxicity observed with irinotecan.








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