Targeting of radioactive platinum-bisphosphonate anticancer drugs to bone of high metabolic activity.

Platinum-based chemotherapeutics exhibit excellent antitumor properties. However, these drugs cause severe side effects including toxicity, drug resistance, and lack of tumor selectivity. Tumor-targeted drug delivery has demonstrated great potential to overcome these drawbacks.

In Vivo Characterization of Platinum(II)-Based Linker Technology for the Development of Antibody-Drug Conjugates: Taking Advantage of Dual Labeling with Pt and Zr.

Linker instability and impaired tumor targeting can affect the tolerability and efficacy of antibody-drug conjugates (ADCs). To improve these ADC characteristics, we recently described the use of a metal-organic linker, [ethylenediamineplatinum(II)], herein called Initial therapy studies in xenograft-bearing mice revealed that trastuzumab--auristatin F (AF) outperformed its maleimide benchmark trastuzumab-mal-AF and the Food and Drug Administration-approved ado-trastuzumab emtansine, both containing conventional linkers. In this study, we aimed to characterize -based ADCs for in vivo stability and tumor targeting using Pt and Zr.