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**Oratecan** is an investigational all-oral oncology regimen comprising irinotecan and the gut-restricted P-glycoprotein inhibitor encequidar methanesulfonate. Encequidar inhibits intestinal P-glycoprotein to reduce drug efflux and enable therapeutically relevant oral exposure to irinotecan and its active metabolite SN-38. Irinotecan is converted to SN-38, which inhibits DNA topoisomerase I, stabilizes DNA cleavage complexes, and causes replication-associated DNA damage. Oratecan was developed through Hanmi Pharmaceutical's Orascovery platform and evaluated in Phase 1 studies in advanced malignancies. ([clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02250157))
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