The successful use of targeted ultrasound contrast agents (USCAs) for qualitative US-based imaging has been shown by several academic and industrial research groups in different animal models. Furthermore, techniques have been developed that enable the in-vivo quantification of targeted microbubbles (MBs). USCAs for quantitative functional and molecular imaging in small animals can be used for a more detailed characterization of new and established disease models and provide quantitative biological insights into the interaction between drug and target or target and disease in living animals. The advantages of such contrast agents in research and development are seen to be as follows: new functional or molecular findings in the complex biology of disease development, these findings can lead to new therapeutic strategies or drug candidates, a better understanding of the treatment effects of new and existing drug candidates, a more sensitive and specific characterization of early treatment effects in living animals, identification of in-vivo biomarkers for translational medicine. Further outcomes are seen in speeding up the evaluation of new drug compounds and in a reduction of the number of animals used for biomedical research.