Abstract: Cardiovascular diseases are the leading cause of death worldwide, and the morbidity rate of these diseases is continuously increasing in China. The occurrence and development of most cardiovascular diseases are associated with the imbalance of vascular homeostasis and adverse vascular remodeling. Exercise protects cardiovascular health and is involved in regulating vascular homeostasis. Based on the cardiovascular protective effect of exercise, in-depth understanding of the molecular mechanism of vascular homeostasis and vascular remodeling is of great guiding significance for exploring the therapeutic drugs for vascular remodeling. In the present article, the molecular mechanism of vascular homeostasis and remodeling based on exercise-induced cardiovascular protection was addressed. Additionally, the potential biological medicine for treating adverse vascular remodeling as well as their development were reviewed. This may provide new direction and theoretical guidance for the research and development of vascular-related drugs.