Cardiovascular disease remains the leading cause of death worldwide and regenerativemedicine is a promising therapeutic option for this disease. We have developed varioustechniques to attenuate the cardiac remodeling and to regenerate cardiovascular systemsvia stem cell application. Besides cell therapy, we are interested in the modulationof pathological inflammation mediated by macrophages in the damaged heart tissueto arouse endogenous reparative responses with biocompatible small molecules. Certainly, current understanding of mechanisms of tissue regeneration will lead to thedevelopment of innovative regenerative medicine for cardiovascular disease.