Milestones in camptothecin research

The discovery of the natural product camptothecin in the early 1960s provided the lead structure for a novel, highly promising class of antitumor agents. Significant progress involving the understanding of the mechanism of action, the drug metabolism, chemistry driven analoging programs and clinical research for dose and schedule optimization led to major breakthroughs in the field. Today, with two successful compounds in clinical practice (irinotecen and topotecan) and more than 10 clinical development programs, the campothecins have reached a very high clinical relevance.