Molecular imaging is a form of nanotechnology that enables the noninvasive examination of biological processes in vivo. Radiopharmaceutical agents are used to target biochemical markers, permitting their detection and evaluation. Early visualization of molecular variations indicative of pathophysiological processes can aid in patient diagnoses and management decisions. Molecular imaging is performed by introducing into the body molecular probes, which are often contrast agents that have been nanoengineered to target and tether to molecules, thus enabling their radiologic identification. Through a nanoengineering process, ultrasound contrast agents can be targeted to specific molecules, extending ultrasound’s capabilities from the tissue to molecular level. Molecular ultrasound, or targeted contrast-enhanced ultrasound (TCEUS), has recently emerged as a popular molecular imaging technique due to its ability to provide real-time anatomic and functional information without ionizing radiation. However, molecular ultrasound represents a novel form of molecular imaging and consequently remains largely preclinical. This review explores the commonalities of TCEUS across several molecular targets and points to the need for standardization of kinetic behavior analysis. The literature underscores evidence gaps and the need for additional research. The application of TCEUS is unlimited but needs further standardization to ensure that future research studies are comparable.