A Population Approach to Evaluate the Parent-Metabolite Pharmacokinetics of a Novel Oral SN38 Prodrug in Rats

Background: Irinotecan hydrochloride and its active metabolite (SN38) function as topoisomerase I inhibitors, with the active metabolite being 100-1000 times more potent. Although irinotecan is widely used as a first-line therapy in metastatic colorectal cancer (mCRC), significant interindividual pharmacokinetic (PK) variability and dose-limiting toxicities restrict its application. We have developed a novel lipid-drug conjugate of […]