DNA topoisomerase is one of drug targets in cancer therapy. Camptothecin is
a plant alkaloid derived from the Chinese tree Camptotheca acuminate. It has been
demonstrated that the plant alkaloid camptothecin (CPT) and its analogs caused DNA
damage by specifically targeting DNA topoisomerase, effectively devastating a broad
spectrum of tumors. Although the anti-tumor activities of CPT and its analogs have
been intensively studied for nearly fifty years, recent advances in drug delivery systems
of CPT have considerably improved this drug’s efficiency and prevented drug
resistance. However, CPT and its analogs showed extremely low water solubility,
inactivation of carboxylate salt, undesired interaction with human serum albumin and
short half-life, therefore, the development of new and effective CPT-derived products is
ongoing. In this chapter, we will summarize the current status of CPT-derived anticancer
drugs in literatures, patents and highlight their clinical application.
Keywords: Aminocamptothecin, anti-tumor efficacy, belotecan, bioavailability,
Camptothecin, cancer, clinical trial, drug delivery system, irinotecan, liposomal
camptothecin, micelles, nanomedicine, nanoparticles, 9-nitrocamptothecin,
pharmaceutical dosage form, pharmacokinetics, poly(ethylene glyclol), polymeric
therapeutics, serum stability, topoisomerase I inhibitor, topotecan, water
solubility.
