Molecular or personalized medicine is the future of patient management and molecular imaging plays a key role towards this goal. Recently, nanoplatform-based molecular imaging has emerged as an interdisciplinary field, which involves chemistry, engineering, biology, and medicine. Possessing unprecedented potential for early detection, accurate diagnosis, and personalized treatment of diseases, nanoplatforms have been employed in every single biomedical imaging modality, namely, optical imaging, computed tomography, ultrasound, magnetic resonance imaging, single-photon-emission computed tomography, and positron emission tomography. Multifunctionality is the key advantage of nanoplatforms over traditional approaches. Targeting ligands, imaging labels, therapeutic drugs, and many other agents can all be integrated into the nanoplatform to allow for targeted molecular imaging and molecular therapy by encompassing many biological and biophysical barriers. In this Review, we will summarize the current state-of-the-art of nanoplatforms for targeted molecular imaging in living subjects.