@article {doi:10.1002/anie.201709532,
	title = {An Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy},
	journal = {Angewandte Chemie International Edition},
	volume = {56},
	number = {46},
	year = {2017},
	pages = {14712-14717},
	abstract = {Abstract The 18-membered macrocycle H2macropa was investigated for 225Ac chelation in targeted alpha therapy (TAT). Radiolabeling studies showed that macropa, at submicromolar concentration, complexed all 225Ac (26 kBq) in 5 min at RT. [225Ac(macropa)]+ remained intact over 7 to 8 days when challenged with either excess La3+ ions or human serum, and did not accumulate in any organ after 5 h in healthy mice. A bifunctional analogue, macropa-NCS, was conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. Both constructs rapidly radiolabeled 225Ac in just minutes at RT, and macropa-Tmab retained >99 \% of its 225Ac in human serum after 7 days. In LNCaP xenograft mice, 225Ac-macropa-RPS-070 was selectively targeted to tumors and did not release free 225Ac over 96 h. These findings establish macropa to be a highly promising ligand for 225Ac chelation that will facilitate the clinical development of 225Ac TAT for the treatment of soft-tissue metastases.},
	keywords = {actinium, CANCER, Chelates, macrocycles, RADIOPHARMACEUTICALS},
	doi = {10.1002/anie.201709532},
	url = {https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201709532},
	author = {Thiele, Nikki A. and Brown, Victoria and Kelly, James M. and Amor-Coarasa, Alejandro and Jermilova, Una and MacMillan, Samantha N. and Nikolopoulou, Anastasia and Ponnala, Shashikanth and Ramogida, Caterina F. and Robertson, Andrew K. H. and Rodr{\'\i}guez-Rodr{\'\i}guez, Cristina and Schaffer, Paul and Williams Jr., Clarence and Babich, John W. and Radchenko, Valery and Wilson, Justin J.}
}
