MFC-1040, Apaxen’s lead compound
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.