HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS		QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Services Email this article to a friend Similar articles in this journal Alert me to new issues of the journal Download to citation manager Google Scholar Articles by Skovronsky, D. PubMed Articles by Skovronsky, D.

Results of multi-center clinical trials comparing four ¹⁸F PET amyloid-imaging agents: Preclinical to clinical correlations

¹ Avid Radiopharmaceuticals, Inc., Philadelphia, Pennsylvania; ² U. Penn, Philadelphia, Pennsylvania; ³ Mayo Clinic, Rochester, Minnesota; ⁴ JHU, Baltimore, Maryland; ⁵ Wash U, St. Louis, Missouri; ⁶ Duke, Durham, North Carolina; ⁷ Wake Forest, Winston-Salem, North Carolina; ⁸ U Mich, Ann Arbor, Michigan; ⁹ Columbia U, New York, New York

133

Objectives: Develop ¹⁸F PET ligands for amyloid plaques in Alzheimer’s disease (AD).

Methods: We have screened more than 200 fluorinated compounds to find an optimal ¹⁸F ligand for PET imaging of amyloid plaques. First results of an exploratory clinical trial with the tracer ¹⁸F-AV-1 (now known as BA94-9172) were previously presented by C. Rowe. Four new ligands, ¹⁸F-AV-19, ¹⁸F-AV-45, ¹⁸F-AV-138, and ¹⁸F-AV-144, were also selected for testing in human trials. We imaged a total of 94 subjects (38 mild to moderate AD and 56 healthy controls, HCs) across 12 centers. With each compound dosimetry, kinetic brain imaging and metabolism were obtained.

Results: All four new compounds were well tolerated, showed acceptable dosimetry and were quickly metabolized. ¹⁸F-AV-45, ¹⁸F-AV-138, and ¹⁸F-AV-144 showed excellent amyloid-imaging properties, with clear separation between AD and HC. Distribution volume ratios and standardized uptake volume ratios were in the range of 1.5 – 2.5 in AD vs. 0.8 – 1.5 in HC. Kinetics of binding and brain washout varied across the compounds, and partially correlated with preclinical evaluations.

Conclusions: Several ¹⁸F-AV-compounds successfully imaged amyloid plaques.

Research Support: Avid Radiopharmaceuticals, Inc., NIH grants (SBIR to DMS; AG-022559 to HFK) *Additional contributors to this work include: Bradley Boeve, Robert Dannals, P. Murali Doraiswamy, Sudha Garg, Bradley Kemp, Mike Kilbourn, David Knopman, Rajesh Manchanda, Ronald Petersen, Michael Pontecorvo, Yaakov Stern, Zhude Tu, Ronald L. Van Heertum

This Article Services Email this article to a friend Similar articles in this journal Alert me to new issues of the journal Download to citation manager Google Scholar Articles by Skovronsky, D. PubMed Articles by Skovronsky, D.