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Non‐invasive, real‐time, dynamic, and quantitative molecular imaging has been developed to facilitate disease diagnosis, drug development, and pathological analysis at the molecular level. Qualitative and quantitative analysis and imaging of physiological processes at the molecular level can be achieved with advanced molecular imaging by employing imaging contrast agents in combination with traditional imaging modalities, such as optical imaging, ultrasound imaging, magnetic resonance imaging, single‐photon emission computed tomography, and positron emission tomography. With the aid of molecular imaging, absorption, distribution, metabolism, excretion, and other processes of drugs in various animals can be monitored quantitatively, and in vivo pharmacokinetics and pharmacodynamics can be simulated before clinical trials, which significantly shorten the period for drug development and reduce the number of animals participating in various tests. Here, the role of molecular imaging in drug target validation, drug screening, drug sensitivity analysis, pharmacokinetics research, drug efficacy evaluation, and other processes of chemical and biological drug research and development is summarized. Molecular imaging has become a powerful and effective tool in the research and development of various drugs for the treatment of a variety of diseases. Advanced molecular imaging can provide important support for disease and drug research, which will accelerate drug discovery and development.
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