Molecular‐Based Magnetic Resonance Multimodal Probes for Tumor Biomarker Imaging

ABSTRACT

Cancer remains a formidable global health challenge, necessitating advanced strategies to mitigate its profound socio‐economic and clinical impacts. Central to cancer progression is the tumor microenvironment (TME), a complex landscape characterized by unique physiological and molecular alterations. These TME biomarkers that can interact with chemical probes offer critical molecular targets for early detection and longitudinal therapeutic monitoring. While magnetic resonance imaging (MRI) is indispensable for clinical diagnostics due to its superior soft‐tissue contrast, its utility is frequently limited by inherently low sensitivity. To overcome these limitations, recent advances have focused on multimodal imaging strategies and TME‐responsive probes. By integrating MRI with complementary imaging modalities, these probes enable the consolidation of multidimensional data—bridging the gap between microscopic molecular recognition and macroscopic in vivo imaging. Although small‐molecule‐based multimodal probes are currently less common than nanoparticle‐based counterparts, they offer distinct advantages in pharmacokinetics and targeting precision. This review systematically summarizes recent design strategies and the transformative potential of small‐molecule responsive probes. We conclude by discussing the future outlook for MR‐based multimodal agents as essential tools for advancing personalized precision oncology.