Gallium: New developments and applications in radiopharmaceutics

Recent progress in the imaging of c‐Met aberrant cancers with positron emission tomography

“…Moreover, the assessment of the studied protein expression, the uptake kinetics, and the pretherapeutic dosimetry may grant a better selection of the treatments as well as monitoring the patient response to the applied therapy and anticipate detection of recurring disease resulting in personalized medicine and radiotheranostic (e.g., probe based on 67/68 Ga). 83 The recent progress in the research field of c-Met based PET imaging here reviewed are highly encouraging, even if the optimization of a PET probe for clinical purposes still faces challenges, suggesting that this family of tracers could be useful as a diagnostic tool for patients selection and for therapeutic applications in the near future.…”

“…The merging of accurate imaging radiotracers with PET will allow noninvasive and real‐time diagnosis of specific cancer types with accurate picture of tumors and metastases and thus precise staging of the disease. Moreover, the assessment of the studied protein expression, the uptake kinetics, and the pretherapeutic dosimetry may grant a better selection of the treatments as well as monitoring the patient response to the applied therapy and anticipate detection of recurring disease resulting in personalized medicine and radiotheranostic (e.g., probe based on 67/68 Ga) 83 …”

Structural Diversity in Divalent Group 14 Triflate Complexes Involving Endocyclic Thia-Macrocyclic Coordination

“…Over the past two decades, there has been an escalation of interest in developing new coordination chemistry of the main group elements, driven by a number of different factors, including the desire for new precursors for the deposition of semiconductor materials for high tech applications, new radiopharmaceuticals for medical imaging and therapy, and metal-free catalysts, as well as intrinsic interest in broadening the types of ligands that form complexes, particularly with the lower oxidation state p-block ions. In contrast to the d-block ions where octahedral coordination predominates, p-block acceptors can display much more variable coordination numbers and geometries, with the structure, denticity, donor type(s), and steric requirements of the ligands significantly influencing the speciation in main group complexes .…”

Bn2DT3A, a Chelator for 68Ga Positron Emission Tomography: Hydroxide Coordination Increases Biological Stability of [68Ga][Ga(Bn2DT3A)(OH)]−

“…19 A more suitable macrocyclic chelator, 1,4,7triazacyclononane-1,4,7-triacetic acid (NOTA, Figure S1), demonstrates the improved radiolabeling efficiency (no heating required) [16][17][18]20 and stability (>98% stable to serum over 2 h) 19,20 that can be obtained by using specifically designed chelators for 68 An area of growing interest in the development of chelators for 68 Ga is the ability to radiolabel the chelator at higher pH values. 8,21,22 This would allow for a simpler radiolabeling process and for the use of targeting moieties that may degrade under acidic conditions, expanding the breadth of diagnostic agents possible using 68 Ga. 22 Some key examples of chelators that have achieved this goal are 4-acetamido-N 1 ,N 7 S1), 23,24 2,2′-{6-[(1-carboxyethyl)amino]-6-phenyl-1,4-diazepane-1,4-diyl}dipropionic acid (DATA PPh , Figure S1), 25 and 2,2′-{ethane-1,2-diylbis[(2-hydroxybenzyl)azanediyl]}diacetic acid (HBED, Figure S1). 12,22,26 These chelators have an acyclic or semicyclic design that improves the coordination kinetics.…”

“…An area of growing interest in the development of chelators for 68 Ga is the ability to radiolabel the chelator at higher pH values. 8 , 21 , 22 This would allow for a simpler radiolabeling process and for the use of targeting moieties that may degrade under acidic conditions, expanding the breadth of diagnostic agents possible using 68 Ga. 22 Some key examples of chelators that have achieved this goal are 4-acetamido- N 1 , N 7 -bis[(3-hydroxy-1,6-dimethyl-4-oxo-1,4-dihydropyridin-2-yl)methyl]-4-(3-{[(3-hydroxy-1,6-dimethyl-4-oxo-1,4-dihydropyridin-2-yl)methyl]amino}-3-oxopropyl)heptanediamide ( THP , Figure S1 ), 23 , 24 2,2′-{6-[(1-carboxyethyl)amino]-6-phenyl-1,4-diazepane-1,4-diyl}dipropionic acid ( DATA PPh , Figure S1 ), 25 and 2,2′-{ethane-1,2-diylbis[(2-hydroxybenzyl)azanediyl]}diacetic acid ( HBED , Figure S1 ). 12 , 22 , 26 These chelators have an acyclic or semicyclic design that improves the coordination kinetics.…”