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) caused DNA damage by specifically targeting DNA topoisomerase, effectively devastating a broad spectrum of tumors. Although the anti-tumoral activity of CPT has been intensively studies for nearly fifty years, recent advances in drug delivery systems of CPT have considerably improved this drug's efficiency. In this review, we will summarize the current status of CPT-derived anti-cancer drugs in literatures and patents and highlight their clinical application.