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Topoisomerase II inhibitors in oncology: an updated patent review (2016-present)
Eleonora Turrini1, Francesca Maffei1, Andrea Milelli1
1Dipartimento di Scienze per la Qualità della Vita, Alma Mater Studiorum, Università di Bologna, Rimini, Italy.
Introduction:
Topoisomerase (topo) II inhibitors continue to represent a promising approach in anticancer therapy, although their clinical application is hampered by drug resistance and dose limiting toxicities.
Area Covered:
We performed a critical analysis of patent literature from January 2016 to January 2025 on topo II inhibitors in oncology using the online databases Espacenet, Wipo, and Google patent.
Expert Opinion:
Substantial progress in the development of novel topo II inhibitors through synthetic chemistry, natural product isolation, molecular modification, and in silico screening was recorded. These compounds belong to different chemical classes and mainly exhibit in vitro cytotoxicity in a low micromolar range, comparable to or greater than that induced by clinically established topo II inhibitors such as doxorubicin and etoposide. Some patented compounds showed catalytic inhibition of topo II enzyme, offering a safer and more effective alternative to topo II poisons. Despite encouraging in vitro data, only a few patents provide in vivo data or mechanistic insights, and none have progressed to clinical trials, highlighting a gap between preclinical innovation and clinical translation. Future research needs advancing in clinical development to fully realize the therapeutic potential of next-generation topo II inhibitors.
Insights
Novel anticancer drugs targeting topoisomerase II (topo II) show promise, with many new compounds exhibiting strong in vitro anticancer activity. However, clinical translation remains a challenge due to limited in vivo data.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Topoisomerase II (topo II) inhibitors are crucial in cancer therapy.
- Clinical use is limited by drug resistance and toxicity.
Purpose of the Study:
- Analyze patent literature on novel topo II inhibitors in oncology.
- Assess preclinical advancements and identify clinical translation gaps.
Main Methods:
- Systematic review of patent databases (Espacenet, Wipo, Google Patent) from 2016-2025.
- Analysis of synthetic chemistry, natural product isolation, and in silico screening approaches.
Main Results:
- Significant progress in developing diverse topo II inhibitors with potent in vitro cytotoxicity.
- Identification of catalytic inhibitors as a potentially safer alternative to topo II poisons.
- Limited in vivo data and absence of clinical trial progression noted.
Conclusions:
- Next-generation topo II inhibitors demonstrate promising preclinical efficacy.
- Advancing clinical development is essential to overcome the innovation-translation gap.
- Future research should focus on in vivo validation and clinical trials.
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