An updated patent review of autotaxin inhibitors (2017–present)

In the past four years, the classification of ATX inhibitors based on binding modes has brought great benefits to the discovery of more efficacious inhibitors. In addition to GLPG1690 currently in phase III clinical studies for IPF, BBT-877, and BLD-0409 as potent ATX inhibitors have been enrolled in phase I clinical evaluation; meanwhile, many effective molecules were also reported successively. However, most emerging ATX inhibitors in the last four years are closely analogs of previous entities, such as GLPG1690 and PF-8380, which translate into the urgently identification of ATX inhibitors with diverse structural features and promising properties in the near future.