The use of monolabeled tumor-targeting peptides for molecular imaging is widespread. However, it is often desirable to use the same compound for different clinical applications, e.g., combined pre- and intraoperative tumor detection. On the basis of their detection sensitivity, the combination of radioactivity and fluorescence is probably the most valuable in multimodal molecular imaging. In this review, we compare multimodal peptide derivatives and discuss the influence of the diagnostic labels on receptor affinity and biodistribution. On the basis of the described constructs, we propose improvements for the design of future multimodal tumor-targeting peptide derivatives.