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. 2023 Oct 13;16(10):1456. doi: 10.3390/ph16101456

Table 1.

Marketed topoisomerase inhibitors.

Sl. Drug Class Mechanism/Target Indications Adverse Drug Reactions Ref.
1 Doxorubicin Anthracycline Topoisomerase IIα and IIβ poison, intercalation, free radicals Various cancers Cardiotoxicity, myelosuppression, nausea, potential for cumulative toxicity [53,54]
2 Epirubicin Anthracycline Topoisomerase IIα and IIβ poison, intercalation, free radicals Breast cancer Cardiotoxicity, myelosuppression, nausea, potential for cumulative toxicity [36]
3 Valrubicin Anthracycline Topoisomerase IIα and IIβ poison, intercalation, free radicals Urinary bladder carcinoma Local irritation, urinary symptoms, myelosuppression [55]
4 Daunorubicin Anthracycline Topoisomerase IIα and IIβ poison, intercalation, free radicals Leukemia Cardiotoxicity, myelosuppression, nausea, potential for cumulative toxicity [56]
5 Idarubicin Anthracycline Topoisomerase IIα and IIβ poison, intercalation, free radicals Leukemia Cardiotoxicity, myelosuppression, nausea, potential for cumulative toxicity [57]
6 Mitoxantrone Anthracenedione Topoisomerase II poison, intercalation Leukemia, prostate cancer, MS Myelosuppression, potential for cumulative toxicity, potential for myelosuppression [58]
7 Pixantrone Anthracenedione Topoisomerase II poison, intercalation Non-Hodgkin B-cell lymphoma Myelosuppression, potential for cumulative toxicity [43]
8 Amsacrine Acridine Topoisomerase II poison, intercalation Acute leukemia Myelosuppression, potential for cumulative toxicity
9 Camptothecin Camptothecin Topoisomerase I inhibitor, DNA strand breaks Not specified Gastrointestinal toxicity, myelosuppression, potential for cumulative toxicity [59]
10 Topotecan Camptothecin Topoisomerase I inhibitor, DNA strand breaks Small-cell lung cancer Myelosuppression, gastrointestinal toxicity, potential for cumulative toxicity [60,61]
11 Irinotecan Camptothecin Topoisomerase I inhibitor, DNA strand breaks Colon and rectal carcinoma Diarrhea, myelosuppression, potential for cumulative toxicity [62]
12 Belotecan Camptothecin Topoisomerase I inhibitor, DNA strand breaks Non-small-cell lung cancer, ovarian cancer Myelosuppression, gastrointestinal toxicity, potential for cumulative toxicity [50]
13 Etoposide Epipodophyllotoxin Topoisomerase II poison, intercalation Testicular tumors, small-cell lung cancer Myelosuppression, gastrointestinal toxicity, potential for cumulative toxicity [63]
14 Teniposide Epipodophyllotoxin Topoisomerase II poison, intercalation Childhood acute lymphoblastic leukemia Myelosuppression, gastrointestinal toxicity, potential for cumulative toxicity [64]