PET Imaging of Antisense Oligonucleotide Distribution Using Click Chemistry

A breakthrough pretargeted PET imaging platform enabling quantitative CNS biodistribution of ASOs.

Publication Title: PET imaging of antisense oligonucleotide distribution in rat and nonhuman primate brains using click chemistry

Authors: Brendon E. Cook, Thomas C. Pickel, Sangram Nag, Philippe N. Bolduc, Rouaa Beshr, Anton Forsberg Morén, Cathy Muste, Di Jiang, Long Yuan, Prodip Datta, Piotr Ochniewicz, Yasir Khani Meynaq, Sac-Pham Tang, Mario Amatruda, Qize Zhang, Jonathan M. DuBois, Armin Delavari, Stephanie K. Klein, Ildiko Polyak, Adebowale Shoroye, Christer Halldin, Laurent Martarello, Emily A. Peterson, and Maciej Kaliszczak 

This publication describes a transformative pretargeted PET imaging strategy that uses bioorthogonal click chemistry to visualize the distribution of antisense oligonucleotides (ASOs) in the CNS. The method separates ASO administration from PET tracer delivery, enabling high-specificity binding, reduced radiation exposure, and accurate quantification across brain regions. The study validates the approach in rodents and non-human primates, including therapeutic ASOs such as BIIB080.

Why Read this Publication:

• Introduces a first-of-its-kind PET methodology for ASO biodistribution.
• Demonstrates specific, covalent in vivo binding enabled by click chemistry.
• Provides robust CNS imaging data across rat and NHP models.
• Enables quantitative evaluation of intrathecal ASO delivery.
• Advances drug-development strategies for RNA-targeting therapeutics.

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