Topotecan, a potent inhibitor of DNA topoisomerase I, has shown cytost
atic activity in preclinical and clinical studies with a great number
of tumors, i.e., ovarian cancer, small-cell (SCLC) and non-small-cell
lung carcinomas (NSCLC), brain tumors. leukemia and pediatric tumors,
especially neuroblastomas, head and neck tumors. colorectal and pancre
atic tumors, and breast cancer. Combination therapies, for example wit
h topoisomerase II inhibitors and other cytostatic agents, have been e
xamined recently. Beyond that, topotecan is effective as a radiosensit
izer and may thus be interesting in combination with radiotherapy. Sev
ere but manageable and reversible myelosuppression, particularly neutr
openia, constitutes the most frequent side effect. Nonhematological gr
ade III or IV toxicities are generally rare.