Development of a radioiodinated apoptosis–inducing ligand rhTRAIL and a radiolabelled agonist TRAIL receptor antibody for clinical imaging studies

摘要

BACKGROUND AND PURPOSEThe TNF-related apoptosis inducing ligand (TRAIL) induces apoptosis through activation of the death receptors, TRAIL-R1 and TRAIL-R2. Recombinant human (rh) TRAIL and the TRAIL-R1 directed monoclonal antibody mapatumumab are currently clinically evaluated as anticancer agents. The objective of this study was to develop radiopharmaceuticals targeting the TRAIL-R1, suitable for clinical use to help understand and predict clinical efficacy in patients.