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Molecules 2018, 23(8), 1929;

In Vivo Brain Imaging, Biodistribution, and Radiation Dosimetry Estimation of [11C]Celecoxib, a COX-2 PET Ligand, in Nonhuman Primates

Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, 1051 Riverside Drive, New York, NY 10032, USA
Now at Department of Radiology, University of Southern California, Los Angeles, CA 90089, USA
Department of Psychiatry, Columbia University, New York 10032, NY, USA
Now at Department of Psychiatry, Stony Brook School of Medicine, Stony Brook, New York, NY 11794, USA
Author to whom correspondence should be addressed.
Received: 9 July 2018 / Revised: 26 July 2018 / Accepted: 27 July 2018 / Published: 2 August 2018
(This article belongs to the Section Medicinal Chemistry)
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COX-2 selective inhibitors (COXIBs) are non-steroidal anti-inflammatory drugs (NSAIDs), with fewer side effects compared with non-selective NSAIDs, and are used for the treatment of arthritis, headaches, and other inflammatory diseases of the brain and peripheral tissues. Radiolabeled COXIBs may permit positron emission tomography (PET) imaging of COX-2 localization and activity in diseases, enable monitoring of inflammatory processes, and determine target occupancy of COX-2 activity by NSAIDs, thus, accelerating the development of novel CIXIBs. We synthesized [11C]celecoxib, one of the COXIBs and a prescription drug, and here report its in vivo uptake in the brain, whole body biodistribution, and radiation dosimetry in baboons using PET. Brain imaging experiments were performed in one baboon and whole body PET scans were performed in triplicates in two male baboons using an ECAT ACCEL (Siemens Medical Solutions, Inc. Knoxville) under anesthetic conditions. PET studies in baboons show that [11C]celecoxib penetrates the blood brain barrier (BBB) and accumulates in the brain, followed by a washout of radioactivity. The liver has the highest residence time and the gallbladder is the critical organ for [11C]celecoxib. Organ Level Internal Dose Assessment (OLINDA) estimates indicate that the maximum permissible single study dosage of [11C]celecoxib in humans is 1110 MBq (30 mCi) for both males and females under the 21 CFR 361.1 dose limit for research subjects. View Full-Text
Keywords: PET; COX-2; celecoxib; dosimetry; biodistribution; brain PET; COX-2; celecoxib; dosimetry; biodistribution; brain

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Kumar, J.S.D.; Bai, B.; Zanderigo, F.; DeLorenzo, C.; Prabhakaran, J.; Parsey, R.V.; Mann, J.J. In Vivo Brain Imaging, Biodistribution, and Radiation Dosimetry Estimation of [11C]Celecoxib, a COX-2 PET Ligand, in Nonhuman Primates. Molecules 2018, 23, 1929.

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