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Tenifatecan (SN2310) is an injectable emulsion formulation of SN-38, which is the active metabolite of the topoisomerase I inhibitor irinotecan. By delivering SN-38 directly in a lipid-based emulsion, tenifatecan is designed to bypass the requirement for hepatic conversion by carboxylesterases, a process that often results in significant inter-patient variability and unpredictable toxicity with irinotecan. As a Topoisomerase I inhibitor, the released SN-38 stabilizes the cleavable complex between DNA and the enzyme, preventing DNA religation and inducing lethal double-strand breaks during the S-phase of the cell cycle. This asset was part of the portfolio of OncoGenex Pharmaceuticals, which merged with Achieve Life Sciences in 2017. It was primarily investigated in Phase 1 clinical trials for patients with advanced solid tumors who had failed conventional therapies.
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