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First-in-human imaging using [11C]MDTC: a radiotracer targeting the cannabinoid receptor type 2.
Du, Yong; Coughlin, Jennifer M; Brosnan, Mary Katherine; Chen, Allen; Shinehouse, Laura K; Abdallah, Rehab; Lodge, Martin A; Mathews, William B; Liu, Chen; Wu, Yunkou; Minn, Il; Finley, Paige; Hall, Andrew W; Lesniak, Wojciech G; Dannals, Robert F; Horti, Andrew G; Pomper, Martin G.
Afiliação
  • Du Y; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Coughlin JM; Department of Psychiatry and Behavioral Sciences, Johns Hopkins Medical Institutions, Baltimore, MD, 21287, USA.
  • Brosnan MK; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Chen A; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Shinehouse LK; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Abdallah R; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Lodge MA; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Mathews WB; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Liu C; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Wu Y; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Minn I; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Finley P; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Hall AW; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Lesniak WG; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Dannals RF; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Horti AG; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA.
  • Pomper MG; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, 601 N. Caroline St., JHOC 3223, Baltimore, MD, 21287, USA. mpomper@jhmi.edu.
Eur J Nucl Med Mol Imaging ; 50(8): 2386-2393, 2023 07.
Article em En | MEDLINE | ID: mdl-36877235
ABSTRACT

PURPOSE:

We report findings from the first-in-human study of [11C]MDTC, a radiotracer developed to image the cannabinoid receptor type 2 (CB2R) with positron emission tomography (PET).

METHODS:

Ten healthy adults were imaged according to a 90-min dynamic PET protocol after bolus intravenous injection of [11C]MDTC. Five participants also completed a second [11C]MDTC PET scan to assess test-retest reproducibility of receptor-binding outcomes. The kinetic behavior of [11C]MDTC in human brain was evaluated using tissue compartmental modeling. Four additional healthy adults completed whole-body [11C]MDTC PET/CT to calculate organ doses and the whole-body effective dose.

RESULTS:

[11C]MDTC brain PET and [11C]MDTC whole-body PET/CT was well-tolerated. A murine study found evidence of brain-penetrant radiometabolites. The model of choice for fitting the time activity curves (TACs) across brain regions of interest was a three-tissue compartment model that includes a separate input function and compartment for the brain-penetrant metabolites. Regional distribution volume (VT) values were low, indicating low CB2R expression in the brain. Test-retest reliability of VT demonstrated a mean absolute variability of 9.91%. The measured effective dose of [11C]MDTC was 5.29 µSv/MBq.

CONCLUSION:

These data demonstrate the safety and pharmacokinetic behavior of [11C]MDTC with PET in healthy human brain. Future studies identifying radiometabolites of [11C]MDTC are recommended before applying [11C]MDTC PET to assess the high expression of the CB2R by activated microglia in human brain.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons combinada à Tomografia Computadorizada Idioma: En Ano de publicação: 2023 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons combinada à Tomografia Computadorizada Idioma: En Ano de publicação: 2023 Tipo de documento: Article