Blood vessels constitute the first organ in the embryo and form the largest network in the body, but sadly are often deadly. Angiogenesis is the process of generating new capillary blood vessels. Vasculogenesis is the term used for spontaneous blood-vessel formation, and intussusceptions is the term for new blood vessel formation by splitting off existing ones. Angiogenesis is a normal and vital process in growth and development, as well as in wound healing and in granulation tissue. It is also a fundamental step in the transition of tumors from a dormant state to a malignant one, leading to the use of angiogenesis inhibitors. Angiogenesis may be a target for combating diseases characterized by either poor vascularisation or abnormal vasculature. Application of specific compounds that may inhibit or induce the creation of new blood vessels in the body may help combat such diseases. In this review, we will present an overview of the knowledge gained in studies related to the identification and characterization of different inhibitors and regulators of angiogenesis and also to highlight briefly the pathological and physiological angiogenesis.