sobuzoxane

Sobuzoxane is an orally bioavailable bisdioxopiperazine derivative that serves as a prodrug for the active metabolite ICRF-154. It acts as a catalytic inhibitor of DNA topoisomerase II, an enzyme essential for DNA replication, transcription, and chromosome segregation. Unlike topoisomerase II poisons such as etoposide, which stabilize the covalent enzyme-DNA cleavable complex and induce double-strand breaks, sobuzoxane inhibits the enzyme's catalytic cycle without directly inducing significant DNA strand breaks. Approved in Japan for the treatment of adult T-cell leukemia/lymphoma (ATL) and other malignant lymphomas, it is frequently utilized in elderly or chemotherapy-intolerant patients due to its relatively mild toxicity profile. It is often incorporated into low-dose palliative or salvage regimens like MTX-HOPE (methotrexate, hydrocortisone, vincristine, sobuzoxane, and etoposide). Additionally, sobuzoxane has been investigated for its potential cardioprotective effects against anthracycline-induced damage, similar to its structural relative dexrazoxane, and can enhance the cytotoxicity of drugs like doxorubicin through the release of formaldehyde during its metabolism.

Brand names

Perazolin

Other names

MSTSBZsobuzoxanum