Human Biodistribution and Dosimetry of the PET Radioligand [11C]Flumazenil (FMZ)

• Published in: Molecular imaging and biology Vol. 14; no. 1; pp. 115 - 122
• Main Authors: Laymon, Charles M., Narendran, Rajesh, Mason, Neale S., Carney, Jonathan P., Lopresti, Brian J., Mathis, Chester A., Mountz, James M., Sashin, Donald, Frankle, W. Gordan
• Format: Journal Article
• Language: English
• Published: New York Springer-Verlag 01.02.2012; Springer Nature B.V
• Subjects: Adult; Blood; Carbon Radioisotopes - chemistry; Carbon Radioisotopes - pharmacokinetics; Dosimetry; Eye lens; Female; Flumazenil - chemistry; Flumazenil - pharmacokinetics; Gonads; Humans; Imaging; Male; Medicine; Medicine & Public Health; Positron-Emission Tomography - methods; Radiation; Radiation Dosage; Radioisotopes; Radiology; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - pharmacokinetics; Research Article; Tissue Distribution; Urinary bladder; Whole Body Imaging - methods; C]Flumazenil; Biodistributiom; Dosimetry; [; Positron emission tomography
• ISSN: 1536-1632; 1860-2002
• DOI: 10.1007/s11307-011-0478-2

Purpose We measure the whole-body distribution of IV injected [ 11 C]Flumazenil (FMZ) as a function of time in adult subjects and determine the absorbed radiation doses. Procedures After injection with 770 MBq of [ 11 C]FMZ (nominal), each of six subjects underwent nine consecutive whole body PET scans. Twelve source organs were identified using PET attenuation and emission images. Activity within each organ as a function of time was determined from the sequence of the nine PET scans. Source organ time activity curves were integrated and normalized by the injected dose to yield source organ residence times for the no voiding situation. Separate bladder residence-time calculations were performed for the cases of a 1- and a 2-h voiding interval. Using the source organ residence times as input, the program OLINDA/EXM (Stabin et al. in J Nucl Med. 46:1023-1027, 2005 ) was used to perform dosimetry calculations for the various body organs and for the whole body. Results For the no voiding situation, the average whole-body radiation equivalent dose was 3.02 × 10 −3  mSv/MBq of injected [ 11 C]FMZ. The average effective dose and effective dose equivalent was 7.57 × 10 −3 and 1.12 × 10 −2  mSv MBq −1 , respectively. The organ receiving the highest equivalent dose was the urinary bladder wall with an average of 6.32 × 10 −2  mSv MBq −1 . Conclusion On average, the administration of less than 790 MBq (21 mCi) of [ 11 C]FMZ yields (no voiding model) an organ equivalent dose of under 50 mSv [the single dose limit for research studies under US regulations (21CFR361.1) to body organs other than blood forming organs, gonads or the lens of the eye] to all organs. Equivalent dose to the blood forming organs and gonads from a 790 MBq administered FMZ dose is well under the 30 mSv limit provided under 21CFR361.1. Additionally, administration of less than 1320 MBq (35.7 mCi) yields an effective dose [International Commission on Radiation Protection (ICRP) 60 tissue weighting scheme] of under 10 mSv, which is the ICRP IIb (minor to intermediate) risk category limit.