Molecular Imaging in the Development of Antibody-Drug Conjugates

Antibody-drug conjugates (ADCs) are novel drugs that deliver a potent cytotoxic payload to the tumor site, by exploiting the specificity of a monoclonal antibody (mAb) to tumor antigens expressed on cancer cells. ADCs allow the delivery of drugs to tumor cells or microenvironment while minimizing toxicity to normal tissue. More than 80 ADCs worldwide are currently under clinical development, of which nine have already received FDA approval. Molecular imaging can play a vital role in evaluating the biodistribution and pharmacokinetics of ADCs for optimal patient selection and early clinical trial development. This chapter provides an overview of ADC structure and design, outlines approved ADCs, discusses the role of molecular imaging in drug development, and highlights clinical and pre-clinical experience with radiolabelled ADCs [1].