RT Journal Article
SR Electronic
T1 Whole-Body Distribution and Radiation Dosimetry of <sup>11</sup>C-Elacridar and <sup>11</sup>C-Tariquidar in Humans
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP 1265
OP 1268
DO 10.2967/jnumed.116.175182
VO 57
IS 8
A1 Bauer, Martin
A1 Blaickner, Matthias
A1 Philippe, Cécile
A1 Wadsak, Wolfgang
A1 Hacker, Marcus
A1 Zeitlinger, Markus
A1 Langer, Oliver
YR 2016
UL http://jnm.snmjournals.org/content/57/8/1265.abstract
AB 11C-elacridar and 11C-tariquidar are new PET tracers to assess the transport activity of P-glycoprotein (adenosine triphosphate–binding cassette subfamily B, member 1 [ABCB1]) and breast cancer resistance protein (adenosine triphosphate–binding cassette subfamily G, member 2 [ABCG2]). This study investigated the whole-body distribution and radiation dosimetry of both radiotracers in humans. Methods: Twelve healthy volunteers (6 women, 6 men) underwent whole-body PET/CT imaging over the 90 min after injection of either 11C-elacridar or 11C-tariquidar. Radiation doses were calculated with OLINDA/EXM software using adult reference phantoms. Results: Biodistribution was consistent with a major elimination route of hepatobiliary excretion, which may be mediated by ABCB1 and ABCG2. High radioactivity uptake was seen in liver, followed by spleen and kidneys, whereas brain uptake was lowest. Effective doses were 3.41 ± 0.06 μSv/MBq for 11C-elacidar and 3.62 ± 0.11 μSv/MBq for 11C-tariquidar. Conclusion: Our data indicate that both 11C-elacridar and 11C-tariquidar are safe radiotracers, for which an injected activity of 400 MBq corresponds to a total effective dose of approximately 1.5 mSv.