Matching chelators to radiometals for radiopharmaceuticals

EW Price, C Orvig - Chemical Society Reviews, 2014 - pubs.rsc.org
Radiometals comprise many useful radioactive isotopes of various metallic elements. When
properly harnessed, these have valuable emission properties that can be used for …

The synthesis and chelation chemistry of DOTA− peptide conjugates

LM De León-Rodríguez, Z Kovacs - Bioconjugate chemistry, 2008 - ACS Publications
Metal complexes of DOTA (1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetraacetic acid)−
peptide conjugates are increasingly used as targeted imaging and therapeutic …

[HTML][HTML] Development of targeted alpha particle therapy for solid tumors

NK Tafreshi, ML Doligalski, CJ Tichacek, DN Pandya… - Molecules, 2019 - mdpi.com
Targeted alpha-particle therapy (TAT) aims to selectively deliver radionuclides emitting α-
particles (cytotoxic payload) to tumors by chelation to monoclonal antibodies, peptides or …

The coordination chemistry of 1, 4, 7, 10-tetraazacyclododecane-N, N′, N ″, N′″-tetraacetic acid (H4DOTA): Structural overview and analyses on structure …

N Viola-Villegas, RP Doyle - Coordination Chemistry Reviews, 2009 - Elsevier
1, 4, 7, 10-Tetraazacyclododecane-N, N′, N ″, N′″-tetraacetic acid (DOTA) is one of the
preeminent carriers of metal-based radiopharmaceutics and imaging contrast agents. This …

Targeted α-therapy: past, present, future?

MW Brechbiel - Dalton Transactions, 2007 - pubs.rsc.org
Monoclonal antibodies have become a viable strategy for the delivery of therapeutic, particle
emitting radionuclides specifically to tumor cells to either augment anti-tumor action of the …

Towards translation of 212 Pb as a clinical therapeutic; getting the lead in!

K Yong, MW Brechbiel - Dalton Transactions, 2011 - pubs.rsc.org
Targeted α-particle therapy offers the potential for more specific tumor cell killing with less
damage to surrounding normal tissue than β-emitters because of the combination of short …

H4octapa-Trastuzumab: Versatile Acyclic Chelate System for 111In and 177Lu Imaging and Therapy

EW Price, BM Zeglis, JF Cawthray… - Journal of the …, 2013 - ACS Publications
A bifunctional derivative of the versatile acyclic chelator H4octapa, p-SCN-Bn-H4octapa, has
been synthesized for the first time. The chelator was conjugated to the HER2/neu-targeting …

α-Particle Radioimmunotherapy of Disseminated Peritoneal Disease Using a 212Pb-Labeled Radioimmunoconjugate Targeting HER2

DE Milenic, K Garmestani, ED Brady… - Cancer biotherapy & …, 2005 - liebertpub.com
These studies demonstrate the feasibility of targeted therapy for the treatment of
disseminated peritoneal disease using 212Pb-labeled Herceptin as an in vivo generator of …

Synthesis and Preclinical Evaluation of Bifunctional Ligands for Improved Chelation Chemistry of 90Y and 177Lu for Targeted Radioimmunotherapy

CS Kang, X Sun, F Jia, HA Song, Y Chen… - Bioconjugate …, 2012 - ACS Publications
We report a practical and high-yield synthesis of a bimodal bifunctional ligand 3p-C-NETA-
NCS containing the isothiocyanate group for conjugation to a tumor targeting antibody. 3p-C …

Preclinical evaluation of NETA-based bifunctional ligand for radioimmunotherapy applications using 212Bi and 213Bi: radiolabeling, serum stability, and …

CS Kang, HA Song, DE Milenic, KE Baidoo… - Nuclear medicine and …, 2013 - Elsevier
INTRODUCTION: Despite the great potential of targeted α-radioimmunotherapy (RIT) as
demonstrated by pre-clinical and clinical trials, limited progress has been made on the …