Clinical use of topoisomerase I inhibitors in anticancer treatment

Med Pediatr Oncol. 2000 Oct;35(4):385-402. doi: 10.1002/1096-911x(20001001)35:4<385::aid-mpo1>;2-e.


The camptothecin analogs topotecan and irinotecan have shown to be among the most effective anticancer agents and, as S-phase specific agents, their antitumor effect is maximized when they are administered in protracted schedules. The documented activity as single agents in many adult and pediatric malignancies has been followed by their use in combination with other anticancer agents. These studies have shown promising results, and have placed topotecan and irinotecan in the first line treatment for some malignancies. However, studies to better determine the optimal schedules and sequence of combinations are needed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Adult
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Camptothecin / analogs & derivatives*
  • Camptothecin / therapeutic use*
  • Child
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Drug Resistance, Neoplasm
  • Enzyme Inhibitors / therapeutic use*
  • Humans
  • Irinotecan
  • Mice
  • Neoplasms / drug therapy*
  • Topoisomerase I Inhibitors*
  • Topotecan / therapeutic use*


  • Enzyme Inhibitors
  • Topoisomerase I Inhibitors
  • Irinotecan
  • Topotecan
  • Camptothecin