Apaxen’s lead compound, MFC-1040, is a novel, first-in-class, orally bioavailable, potent and selective small molecule inhibitor of the biological effects of both intracellular and extracellular MIF.

Effects of blocking MIF biological activity with MFC-1040:

• Reduced tissue remodelling and fibrosis
• Reduced NLRP3 inflammasome activation
• Reduced migration of pro-inflammatory immune cells to inflamed tissue
• Reduced levels of pro-inflammatory cytokines and chemokines
• Enhanced efficacy of (endogenous) corticosteroid-steroids

As a first step towards treatment of the many inflammatory and auto-immune diseases that depend on prolonged MIF activity, MFC-1040 is being developed for treatment of pulmonary inflammatory and fibrotic diseases.

MFC-1040 has shown robust in vivo efficacy in multiple rodent models of Pulmonary Fibrosis, Pulmonary Arterial Hypertension (J. Med. Chem. 2018, 61, 2725-2736), (Int. J. Mol. Sci. 2018, 19, 4105), Neutrophilic Asthma and Gout.

Pre-clinical development of MFC-1040 has been completed. Apaxen expects to start first-in-human (FIH) clinical trials for MFC-1040 by early 2024.