Abstract
CD38 is an established biomarker for the diagnosis and treatment of various malignancies, including multiple myeloma. Accurate assessment of CD38 expression holds significant clinical value for optimizing CD38-targeted therapies. This study developed a series of small-molecule radiotracers for in vivo assessment of CD38 expression and monitoring of therapeutic response. All 68Ga-labeled radiotracers exhibited high radiochemical purity and stability both in vitro and in vivo. PET/CT imaging showed that 68Ga-NOTA-MK0159 uptake in multiple myeloma models correlated positively with CD38 expression and could be blocked by excess MK-0159. Notably, daratumumab did not block the uptake of 68Ga-NOTA-MK0159 under the experimental conditions of this study, suggesting the probe’s potential for assessing CD38 expression during daratumumab therapy. Preclinical studies demonstrated that 68Ga-NOTA-MK0159 enables noninvasive whole-body assessment of CD38 in multiple myeloma, which may guide personalized treatment and monitor CD38 expression during daratumumab therapy.
文章链接：https://pubs.acs.org/doi/10.1021/acs.jmedchem.5c03340
