Radiopharmaceutical therapies are evolving rapidly, offering unprecedented opportunities for targeted tumor eradication, but these innovations come with unique safety challenges. The therapeutic potential of these agents depends on precise molecular targeting, optimal payload selection, controlled biodistribution, and accurate radiation dosing. Small variations in molecular design or pharmacokinetics can dramatically affect efficacy and off-target toxicity, making the design process both a scientific and clinical imperative.

This workshop will delve into insights regarding:

• Leveraging tumor biology, receptor expression, and disease-specific molecular pathways to optimize targeting moieties and payload combinations, improving selectivity and therapeutic index
• Understanding molecular, cellular, and organ-level toxicity mechanisms across radiopharmaceutical modalities, and implementing chemical, formulation, or dosing strategies to minimize adverse effects
• Using preclinical pharmacology, predictive simulations, and early human data to guide rational candidate selection, optimize safety margins, and accelerate clinical translation

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Outcome – Development of a framework for safer tumor-targeted radiopharmaceutical design, integrating molecular targeting, payload selection, and toxicity mitigation strategies to guide candidate prioritization and accelerate preclinical-to-clinical translation.