Breast cancer is increasing at an alarming rate in women around the world, where medical biology is confronted by this disease on two crucial fronts. The first step is the early accurate diagnosis, which is very critical and the second step involves the appropriate clinical management. The current trend in molecular imaging of breast cancer provides not only an excellent tool in diagnosing the disease but also useful in validating the potentiality targeted of a pharmaceutical interventions. This review addresses the effectiveness of imaging technologies to resolve the molecular characterization and pathological evidences in breast cancer. The focus is on the present practices in breast cancer imaging, specifically targeting cellular machineries such as hormone receptors and angiogenic factors.