HIT | Lead optimization | Clinical Candidate | GLP tox | CMC | Ph1 | Ph2 |
---|---|---|---|---|---|---|
PO
|
NuPulin is an oral formulation of HY209 that modulates GPCR19-P2X7 signaling to inhibit the activation of the NLRP3 inflammasome, and is currently being developed as a novel therapeutic agent for idiopathic pulmonary fibrosis (IPF).
Idiopathic pulmonary fibrosis (IPF) is a disease characterized by progressive loss of lung function due to fibrosis and inflammation, leading to symptoms such as shortness of breath and coughing. Current IPF treatments rely on anti-fibrotic agents such as pirfenidone and nintedanib, which primarily aim to slow the progression of fibrosis. However, there is a lack of therapeutic strategies targeting the underlying inflammatory responses. NuPulin is being developed as a differentiated therapy that targets the NLRP3 inflammasome to suppress inflammation and prevent pulmonary fibrosis.
In a bleomycin-induced pulmonary fibrosis animal model, oral administration of HY209 for 14 days resulted in a reduction of inflammation in lung tissue and suppression of fibrosis. In addition, analysis of bronchoalveolar lavage fluid (BALF) showed decreased expression of pro-inflammatory cytokines, inhibition of fibroblast activation, and protective effects on lung tissue.
A Phase 1 clinical trial is currently underway in healthy volunteers. Based on safety data from the single-dose administration, the study is now evaluating the safety and tolerability of repeated dosing.
Respir Res. 2018; 19: 205
Mil Med Res. 2022; 9: 53
Int J Mol Sci. 2023; 24(3): 149