Drug/Small Molecule:

topotecan

An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA topoisomerases, type I. PubChem (source: Drug Bank)

For the treatment of metastatic carcinoma of the ovary and small cell lung cancer following the failure of first-line chemotherapy. (source: Drug Bank)

Topotecan has the same mechanism of action as irinotecan. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. The cytotoxicity of topotecan is thought to be due to double strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topotecan, topoisomerase I and DNA. Mammalian cells cannot efficiently repair these double strand breaks. (source: Drug Bank)

Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the <i>Camptotheca acuminata</i> tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. Topotecan interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other effects may also occur. Unlike irinotecan, topotecan is found predominantly in the inactive carboxylate form at neutral pH and it is not a prodrug. (source: Drug Bank)

Topotecan undergoes a reversible pH dependent hydrolysis of its lactone moiety; it is the lactone form that is pharmacologically active. (source: Drug Bank)

35% (source: Drug Bank)

The primary anticipated complication of overdosage would consist of bone marrow suppression. (source: Drug Bank)

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