ITD-1 is a selective small molecule inhibitor of the TGF-β type I receptor (ALK5), which blocks the TGF-β signaling pathway involved in fibrosis and cell proliferation regulation. It is primarily investigated for its potential therapeutic applications in cardiovascular diseases, showing promise in reducing cardiac fibrosis, promoting cardiomyocyte regeneration, and improving heart function in conditions such as heart failure. Its applications are significant in preclinical studies for developing novel treatments for chronic heart diseases, where modulation of inflammatory, fibrotic, and regenerative processes is essential. Research continues to explore its efficacy and safety in clinical settings.