A patent review of topoisomerase 1 inhibitors (2021-present)

Among the different topoisomerases, essential enzymes that play an important role in DNA processes such as replication and transcription, type I enzymes are targets of particular clinical importance for anticancer and antiparasitic drugs. Bearing this in mind, in the last 5 years specific inhibitors, both poison and suppressor types, have been patented for this target.

This review covers the patent literature on topoisomerase 1 inhibitors and their application published between late 2020-present.

TOP1 inhibitors are being used in combination with synergistic therapies within a multimodal approach, including targeted therapies, adaptive immunotherapy, and the blockade of DNA repair mechanisms. Advances in drug delivery systems, especially antibody-drug conjugates (ADCs), are revolutionizing chemotherapy by enabling localized and tumor-specific drug release. In addition to traditional inhibitors like irinotecan and topotecan, new agents such as deruxtecan and govitecan have been approved, expanding therapeutic options. Moreover, small new molecules with more promising clinical potential are being developed.