Products Cited in Publications Worldwide CD38‐Specific Gallium‐68 Labeled Peptide Radiotracer Enables Pharmacodynamic Monitoring in Multiple Myeloma with PET

CD38‐Specific Gallium‐68 Labeled Peptide Radiotracer Enables Pharmacodynamic Monitoring in Multiple Myeloma with PET

Ajay Kumar Sharma; Kuldeep Gupta; Akhilesh Mishra; Gabriela Lofland; Ian Marsh; Dhiraj Kumar; Gabriel Ghiaur; Philip Imus; Steven P. Rowe; Robert F. Hobbs; Christian B. Gocke; Sridhar Nimmagadda

DOI:

Abstract

The limited availability of molecularly targeted low-molecular-weight imaging agents for monitoring multiple myeloma (MM)-targeted therapies has been a significant challenge in the field. In response, a first-in-class peptide-based radiotracer, [68Ga]Ga-AJ206, is developed that can be seamlessly integrated into the standard clinical workflow and is specifically designed to noninvasively quantify levels and pharmacodynamics by positron emission tomography (PET). A bicyclic , AJ206, is synthesized and exhibits high affinity to (KD: 19.1 ± 0.99 × 10−9 m) by surface plasmon resonance. Further, [68Ga]Ga-AJ206-PET shows high contrast within 60 min and suitable absorbed dose estimates for clinical use. Additionally, [68Ga]Ga-AJ206 detects expression in cell line-derived xenografts, patient-derived xenografts (PDXs), and disseminated disease models in a manner consistent with flow cytometry and immunohistochemistry findings. Moreover, [68Ga]Ga-AJ206-PET successfully quantifies pharmacodynamics in PDXs, revealing increased expression in the tumor following all-trans (ATRA) therapy. In conclusion, [68Ga]Ga-AJ206 exhibits the salient features required for clinical translation, providing CD38-specific high-contrast images in multiple models of MM. [68Ga]Ga-AJ206-PET could be useful for quantifying total levels and pharmacodynamics during therapy to evaluate approved and new therapies in MM and other diseases with involvement.

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Fmoc-NH-PEG4-CH2CH2COOH

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