1.Strategy - selective Target X inhibitor

Target X is involved in a variety of physiological and pathological processes such as inflammatory responses and immune regulation by regulating cytokine secretion, cell migration and adhesion in macrophages and dendritic cells.
Target X is the key mediator for the secretion of multiple inflammatory cytokines andis closely associated with Autoimmune and Fibrotic
Abnormal expression or dysregulation of target X has been closely linked to a number of human diseases, including fibrotic disorders, atherosclerosis, and autoimmune disease.
Target X is widely expressed, and rarely expressed in normal tissues, but highly expressed in pathological tissue (glomerulus, rheumatoid arthritis, and renal interstitial fibrosis).
Autoimmune disorders are characterized by aberrant T cell and B cell reactivity to the body’s own components, resulting in tissue destruction and organ dysfunction.
Target X-facilitated cellular functions include cell migration,survival, proliferation, differentiation, and remodelling of extracellular matrices.
Blockade Target X is a potential treatment strategy for Autoimmune and Fibrotic

2. Results and Data

Asset048 could reduce the inflammatory infiltration, and arthritis score,and relieve joint symptoms.
Asset048 could significantly relieve Kindey pathological changes, Splenic and Lymph node enlargement, and vascular invasion.
Spontaneous Lupus in NZB/W F1 Mice Model-undergoing
Asset048 could prolong the survival of mice and be safer than Prednisone (PNS).
Collagen-induced Arthritis Mice Model
Asset048 hadan obvious relief effect on the joint symptoms of mice, which was better than methotrexate.
unilateral ureteral obstruction (UUO)-induced Renal fibrosis mice model-undergoing
Acceptable PK profile:
The metabolites produced in each incubation system were less than 2.0%.
The bioavailability of dogs is 18.7%.
Good safety profile:
Low cytotoxicity; no hERG inhibition; no genotoxicity;
No animal mortality;
No toxic effects on main organs.