orotecan

Orotecan is an oral formulation of irinotecan hydrochloride being developed by Edison Oncology. It acts as a prodrug that is converted into its active metabolite, SN-38, which inhibits topoisomerase I. This inhibition prevents the religation of DNA strands during replication, leading to lethal double-strand breaks and subsequent cell death. Orotecan is primarily being investigated for the treatment of pediatric sarcomas, recurrent pediatric solid tumors, and various adult malignancies. The drug has undergone a pilot pharmacokinetic study (VAL413) in pediatric patients to evaluate its safety and metabolic profile compared to traditional intravenous administration.

Brand names

Orotecan

Other names

oral irinotecan HClirinotecan hydrochloride