Autotaxin inhibitors: an updated patent review (2021-present)

Autotaxin (ATX) inhibition has attracted considerable interest as a therapeutic strategy, resulting in more than 50 patents being published by various institutions over the past five years. Consequently, a review of these patented compounds and related research progress could facilitate the discovery of novel ATX inhibitors.

This review summarizes ATX inhibitors disclosed in patents from September 2020 to Jan 2026, identified from Espacenet and SciFinder using keyword 'Autotaxin,' and highlights structural features and biological activities in vitro and in vivo.

Currently, beyond the Phase II candidates PAT409 and HW021199, ATX inhibitors FTP-198 and HNC1058 have entered Phase I clinical trials for pulmonary fibrosis, while IOA-289 and HNC664 have advanced to clinical studies for solid tumors, underscoring the immense therapeutic potential of ATX. Although the identification of type V and VI ATX inhibitors has broadened the design landscape, most emerging entities since 2020 remain analogs of GLPG1690 and PAT409, presumably being attributed to the unavailable data of most clinical candidates, and despite the absence of approved drugs, the continued evolution of drug design strategies and application of novel technologies would further facilitate the discovery of ATX candidates, ultimately offering more therapeutic options for patients.