Abstract

Preclinical evaluation constitutes an essential and integral component of the development process of radiopharmaceuticals (RPs). Advances achieved over recent decades in the fields of biology, molecular imaging, radiochemistry, and pharmaceutical chemistry have enabled the development of next-generation targeted RPs capable of delivering radioisotopes to specific cellular and molecular targets. These developments have significantly increased the need for comprehensive preclinical assessment of radiolabeled molecules, particularly with respect to their biodistribution, pharmacokinetics, target specificity, dosimetry, and toxicity profiles. This review discusses current advances in targeted RPs and highlights the fundamental preclinical research parameters involved in their development. In particular, the critical role of biodistribution studies in preclinical evaluation is emphasized in terms of target tissue uptake, normal organ distribution, dosimetry, therapeutic efficacy, and safety assessment.