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Biodistribution and Radiation Dosimetry of ¹¹C-WAY100,635 in Humans

¹ Division of Brain Imaging, Department of Neuroscience, New York State Psychiatric Institute, New York, New York
² Department of Psychiatry, Columbia University College of Physicians and Surgeons, New York, New York
³ Department of Radiology, Columbia University College of Physicians and Surgeons, New York, New York
⁴ Department of Radiology and Radiological Sciences, Vanderbilt University, Nashville, Tennessee

Serotonin 1A receptors have been implicated in a variety of conditions including depression, suicidal behavior, and aggression. Dose estimates for current human studies are based on data from rat dosimetry studies. We report the biodistribution and dosimetry of the PET serotonin 1A antagonist ¹¹C-WAY100,635 in humans. Methods: PET studies of 6 healthy human volunteers (3 male, 3 female) were acquired after a bolus injection of ¹¹C-WAY100,635. Transmission scans of 3.5 min were obtained at each bed position before injection, and emission scans then were collected in 2-dimensional mode over 8 bed positions. Regions of interest were drawn around the brain, left and right lungs, heart, liver, stomach wall, gallbladder, left and right kidneys, spleen, and urinary bladder. Because no fluid was removed from the subjects, whole-body radioactivity was calculated using the injected dose and a calibration factor determined from a cylinder phantom. The area under the curve for each region of interest was determined by trapezoidal integration of the first 3 points, with subsequent points fit by a decreasing monoexponential. The area under the curve was then divided by counts in the whole body, and the resulting residence times were entered into the MIRDOSE3 program. Results: Primary elimination was via kidneys to the urinary bladder. There were no sex differences in organ residence times. The urinary bladder wall was the organ with the highest estimated radiation dose (1.94 x 10^–1 ± 3.57 x 10^–2 mGy/MBq). Except for the kidney and bladder wall, correlation was good between human dosimetry estimates and estimates reported previously from rats. The human dosimetry was 6.6 and 60.6 times higher in the kidneys and urinary bladder wall, respectively, than estimates from rats. Conclusion: The urinary bladder wall is the critical organ for ¹¹C-WAY100,635 in humans. In the United States, according to Radioactive Drug Research Committee guidelines a single dose cannot exceed 300 MBq in a man and 227 MBq in a woman, with up to 3 such injections permitted per annum.

Key Words: PET • serotonin • serotonin 1A

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