Comprehensive SummaryIn recent years, magnetic nanoparticles (MNPs) have received great attention within the field of biomedicine, especially for cancer therapy. This is because MNPs have many excellent physical and chemical properties to provide sufficient imaging information along with satisfactory therapeutic efficacy. Moreover, by virtue of various modification strategies, the obtained multifunctional MNPs can further achieve synergized multimodal cancer theranostic, which is worthy of further study. In this review, we summarize the recent developments in imagingāguided strategies and synergistic cancer therapy based on multifunctional MNPs. Then, we discuss the challenge and perspective of the next generation of MNPsābased imagingāguided cancer therapy, hoping to provide guidance in potential applications.