• Vol. 27 No. 5, 683–687
  • 15 September 1998

Topoisomerase-I Inhibitors in Gynaecologic Tumours



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Topoisomerase inhibitors have been studied using various dose schedules in the treatment of refractory or recurrent gynaecologic cancers. Response rates are between 13% and 20%. Main toxic effects are haematologic and gastrointestinal. The latter remains problematic. Radiotherapy, alkylate, platinum analogs and topoisomerase II inhibitors are currently being studied in combination with camptothecins.

Topoisomerases are essential nuclear enzymes with a multiplicity of cellular functions involving DNA replication, RNA transcription, mitosis, and chromosome condensation. Two classes have been identified: the class I topoisomerases, named “I” because they induce single-strand breaks and reunions of the DNA double helix, and the class II topoisomerases, named “II” because they induce double-strand breakage and reunion reactions within the DNA double helix.

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