Abstract

The process of new drug discovery and development is a lengthy, high-risk, and costly task. Fluorescent molecular imaging (FMI) has tremendous potential for improving the efficiency of drug screening, evaluating drug effects, accelerating the process, and markedly reducing the cost of new drug development from initial target validation and high-throughput screening identification campaigns to the final human translation phases. FMI can help evaluate the role of new candidate drugs under the influence of complex biological responses in living subjects and better understand the mechanism between drug activity and disease, which can help select candidates that seem most likely to succeed or prevent the development of drugs that seem to fail in the end. Hence, in this chapter, FMI was described for its application in drug discovery, including identification of tumor-specific markers, candidate drug screening, determination of pharmacokinetics of drugs, and preparation of prodrugs.

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