firtecan

Firtecan, also known as SN-38, is the active metabolite of the chemotherapy drug irinotecan. It functions as a potent inhibitor of DNA topoisomerase I, an enzyme crucial for DNA replication and transcription. Firtecan exerts its antineoplastic effects by binding to and stabilizing the topoisomerase I-DNA complex, which prevents the re-ligation of DNA strands. This interference leads to DNA breaks, arrests the cell cycle in the S phase, and ultimately induces apoptosis (programmed cell death) in cancer cells. Firtecan is significantly more cytotoxic than its prodrug, irinotecan. Due to its poor aqueous solubility, firtecan is often formulated into drug delivery systems, such as polymer nanoparticles (e.g., SNB-101), to improve its pharmacokinetic profile and therapeutic efficacy. It is currently under development for various solid tumor indications, including small cell lung cancer, pancreatic cancer, and gastric cancer.

Other names

SN-38SN38SN 387-Ethyl-10-hydroxycamptothecin