Class/mechanism: Topoisomerase I inhibitor. Topotecan binds to the topoisomerase I-DNA complex and prevents the religation of single strand breaks that were originally created by topoisomerase I. This leads to double strand DNA damage, which results in cell damage and cell death.
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Diseases for which it is used
- Cervical cancer
- CNS lymphoma
- Diffuse large B-cell lymphoma
- Ewing's sarcoma
- Ovarian cancer
- Small cell lung cancer
- Endometrial cancer
Patient drug information
- Topotecan (Hycamtin) patient drug information (Chemocare)
- Topotecan (Hycamtin) patient drug information (UpToDate)
History of changes in FDA indication
- 5/28/1996: Initial FDA approval for metastatic carcinoma of the ovary after failure of initial or subsequent chemotherapy.
- 11/30/1998: Indication expanded to include small cell lung cancer sensitive disease after failure of first-line chemotherapy. In clinical studies submitted to support approval, sensitive disease was defined as disease responding to chemotherapy but subsequently progressing at least 60 days (in the phase 3 study) or at least 90 days (in the phase 2 studies) after chemotherapy.
- 6/14/2006: Indication expanded to include stage IV-B, recurrent, or persistent carcinoma of the cervix which is not amenable to curative treatment with surgery and/or radiation therapy.