The growing complexity of modern pathology demands integrated approaches that unify diagnosis, targeted treatment, and real-time monitoring, driving the urgent need for a comprehensive understanding of theragnostic nanoplatforms. This review consolidates current advancements to clarify their pivotal role in advancing precision medicine and overcoming limitations of conventional, disjointed therapeutic strategies. We systematically examine the design and synthesis strategies of multifunctional nanoplatforms, detailing core targeting mechanisms and the enabling of key imaging modalities such as magnetic resonance imaging (MRI), positron emission tomography (PET), fluorescence, and photoacoustics. The review further explores the diverse therapeutic payloads—including small molecules, nucleic acids, radionuclides, and photosensitizers—that these platforms deliver, alongside the innovative stimuli-responsive systems for controlled release. Critical analysis is provided on their integration with digital pathology for quantitative monitoring and an overview of promising clinical studies. The significant challenges hindering clinical translation, encompassing regulatory, technical, and economic barriers, are also discussed. Future progress hinges on translating multifunctional laboratory designs into robust, scalable, and clinically viable constructs, while simultaneously establishing standardized frameworks for safety, efficacy, and seamless integration into diagnostic and therapeutic workflows.

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