It is a small molecule, ATP-competitive kinase inhibitor. The compound is characterized by an exquisite selectivity for its target. This target has been validated with KO-mice in models of lung and kidney fibrosis.
FIB992-079 doesn’t inhibit any other unrelated kinase enzyme when tested in a very large kinase panel. The compound also has very favourable binding kinetics, with a fast on-rate and a very slow off-rate. With biomarker assays we have proven that the compound after a single oral dose blocks the target for about 12 hours in multiple tissues. The compound shows fast absorption and high plasma levels after oral administration in multiple species. It is not a CYP-450 inducer neither blocker. It has tested negative in a panel of genotoxoicity assays. In pharmacological in vivo models of lung and kidney fibrosis, performed under the most challenging conditions, it has shown promising signs of in vivo activity.
FIB992-079 is currently under preclinical development and is planned to enter FiH in 2024, followed by phase 2 POC-clinical trials in 2025.