@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.}
}
@article {GRISWOLD2016366,
	title = {Large scale accelerator production of 225Ac: Effective cross sections for 78{\textendash}192MeV protons incident on 232Th targets},
	journal = {Applied Radiation and Isotopes},
	volume = {118},
	year = {2016},
	pages = {366 - 374},
	abstract = {Actinium-225 and 213Bi have been used successfully in targeted alpha therapy (TAT) in preclinical and clinical research. This paper is a continuation of research activities aiming to expand the availability of 225Ac. The high-energy proton spallation reaction on natural thorium metal targets has been utilized to produce millicurie quantities of 225Ac. The results of sixteen irradiation experiments of thorium metal at beam energies between 78 and 192MeV are summarized in this work. Irradiations have been conducted at Brookhaven National Laboratory (BNL) and Los Alamos National Laboratory (LANL), while target dissolution and processing was carried out at Oak Ridge National Laboratory (ORNL). Excitation functions for actinium and thorium isotopes, as well as for some of the fission products, are presented. The cross sections for production of 225Ac range from 3.6 to 16.7mb in the incident proton energy range of 78{\textendash}192MeV. Based on these data, production of curie quantities of 225Ac is possible by irradiating a 5.0gcm-2 232Th target for 10 days in either BNL or LANL proton irradiation facilities.},
	keywords = {Ac, actinium, Alpha-emitting, Ba, Ce, MO, Proton irradiation, RADIOTHERAPY, Th, Thorium},
	issn = {0969-8043},
	doi = {https://doi.org/10.1016/j.apradiso.2016.09.026},
	url = {http://www.sciencedirect.com/science/article/pii/S0969804316307795},
	author = {J.R. Griswold and D.G. Medvedev and J.W. Engle and R. Copping and J.M. Fitzsimmons and V. Radchenko and J.C. Cooley and M.E. Fassbender and D.L. Denton and K.E. Murphy and A.C. Owens and E.R. Birnbaum and K.D. John and F.M. Nortier and D.W. Stracener and L.H. Heilbronn and L.F. Mausner and S. Mirzadeh}
}
