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Ligand Design For Enhanced Complexation Kinetics
One of the most important features of chelating agents intended for nuclear medicine applications is the requirement that complexation with the isotope occurs rapidly and under mild conditions. This is especially important for the emerging applications in PET imaging where isotopes such as Cu-64 have a relatively short half-life and must be quickly incorporated into the contrast agent in order to be efficacious. Macrocyclics is actively exploring new ligand systems to meet these needs and has successfully developed promising new agents through our collaboration with MDS Nordion.
Tircso, G.; Tircsone, E. B.; Suh, E. H.; Jurek, P.; Kiefer, G. E.; Sherry, A. D.; KovaÌ, Z. n., (S)-5-(p-Nitrobenzyl)-PCTA, a Promising Bifunctional Ligand with Advantageous Metal Ion Complexation Kinetics. Bioconjugate Chemistry 20
Contrast Agents for Magnetic Resonance Imaging and Spectroscopy
Macrocyclics was originally founded on contrast agent technologies that were developed in the lab of Professor A. Dean Sherry. The company maintains an active involvement with the development of new lanthanide based contrast agents that show promise for mapping physiological processes such as pH and glucose concentration. In particular, the new PARACEST contrast agents pioneered by Professor Sherry are now part of the company’s offering.
Woods, M.; Caravan, P.; Geraldes, C. F. G. C.; Greenfield, M. T.; Kiefer, G. E.; Lin, M.; McMillan, K.; Prata, M. I. M.; Santos, A. C.; Sun, X.; Wang, J.; Zhang, S.; Zhao, P.; Sherry, A. D., The Effect of the Amide Substituent on the Biodistribution and Tolerance of Lanthanide(III) DOTA-Tetraamide Derivatives. Investigative Radiology 2008, 43, (12), 861-870.
Wu, Y.; Zhou, Y.; Ouari, O.; Woods, M.; Zhao, P.; Soesbe, T. C.; Kiefer, G. E.; Sherry, A. D., Polymeric PARACEST Agents for Enhancing MRI Contrast Sensitivity. Journal of the American Chemical Society 2008, 130, (42), 13854-13855.
Adair, C.; Woods, M.; Zhao, P.; Pasha, A.; Winter, P. M.; Lanza, G. M.; Athey, P.; Sherry, A. D.; Kiefer, G. E., Spectral Properties of a Bifunctional PARACEST Europium Chelate: An Intermediate for Targeted Imaging Applications. Contrast Media & Molecular Imaging 2007, 2, 55-58.
Macrocyclics develops IP based on internal discoveries as well as for customer sponsored programs.
Lanthanide-Based Optical Imaging Probes
The lanthanide series of metals has proven to valuable tools for many applications as a result of their luminescent properties. We have undertaken the development of several new ligands that have shown promise for the ability to generate sensitized luminescence. The goal of this work is to generate bifunctional luminescent probes that can be used for targeted optical imaging.
New chelating agents for PET imaging
PET imaging is clearly one of the fastest growing modalities in nuclear medicine. Until recently F-18 has been the only readily available isotope which has limitations with respect to chemistry and half life. New isotopes such as Cu-64, Ga-68, and Zr-89 are now becoming available which will no doubt expand the capabilities of PET. For this reason Macrocyclics has an active program to develop new bifunctional ligands that are designed specifically for these new isotopes and make them available to our customers.
Perk, L. R.; Vosjan, J. W. D.; Visser, G. W. M.; Budde, M.; Juerek, P.; Kiefer, G. E.; van Dongen, G. A. M. S., p-Isothiocyanatobenzyl- desferrioxamine: A New Bifunctional Chelate for Facile Radiolabelong of Monoclonal Antibodies with 89Zr for Immuno-PET Imaging. European Journal of Nuclear Medicine and Molecular Imaging 2009.
Ferreira, C. L.; Yapp, D. T.; Lamsa, E.; Gleave, M.; Bensimon, C.; Jurek, P.; Kiefer, G. E., Evaluation of Novel Bifunctional chelates for the Development of 64Cu-Based Radiopharmaceuticals. Nuclear Medicine and Biology 2008, 35, 875-882.