Drug intelligence / Profile preview

Oratecan

Development stage
Unknown
Lead developer
Athenex
Modality
Small Molecules
Administration
Oral
01

Overview

**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))

Brand names
Oratecan
Other names
encequidar methanesulfonate + irinotecanirinotecan + encequidarOral IrinotecanOratecan
02

Targets

ABCB1 (P-glycoprotein)TOP1 (DNA Topoisomerase I)

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