Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications

Eduardo Aluicio-Sarduy; Nikki A. Thiele; Kirsten E. Martin; Brett A. Vaughn; Justin Devaraj; Aeli P. Olson; Todd E. Barnhart; Justin J. Wilson; Eszter Boros; Jonathan W. Engle

doi:10.1002/chem.201905202

Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications

Eduardo Aluicio-Sarduy, Nikki A. Thiele, Kirsten E. Martin, Brett A. Vaughn, Justin Devaraj, Aeli P. Olson, Todd E. Barnhart, Justin J. Wilson, Eszter Boros, Jonathan W. Engle

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

Abstract

We report the first targeted nuclear medicine application of the lanthanum radionuclides ^132/135La. These isotopes represent a matched pair for diagnosis via the positron emissions of ¹³²La and therapy mediated by the Auger electron emissions of ¹³⁵La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides. The 18-membered macrocycle, macropa, bound ^132/135La with better molar activity than DO3Apic under similar conditions. These chelators were conjugated to the prostate-specific membrane antigen (PSMA)-targeting agent DUPA to assess the use of radiolanthanum for in vivo imaging. The ^132/135La-labeled targeted constructs showed high uptake in tumor xenografts expressing PSMA. This study validates the use of these radioactive lanthanum isotopes for imaging applications and motivates future work to assess the therapeutic effects of the Auger electron emissions of ¹³⁵La.

Original language	English
Pages (from-to)	1238-1242
Number of pages	5
Journal	Chemistry - A European Journal
Volume	26
Issue number	6
DOIs	https://doi.org/10.1002/chem.201905202
State	Published - Jan 27 2020
Externally published	Yes

Funding

Research reported in this publication was supported in part by the National Cancer Institute of the National Institutes of Health under Award Number T32CA009206 (E.A.S.). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. B.A.V. and K.E.M. acknowledge support through the SBU Chemistry-Biology interface training program (T32GM092714). E.B. acknowledges a Pathway to Independence Award (HL125728) and Stony Brook University for startup funds. J.J.W. thanks the College of Arts and Sciences at Cornell University for financial support of this research.

Funders	Funder number
College of Arts and Sciences at Cornell University
SBU Chemistry-Biology interface training program	T32GM092714
National Institutes of Health
National Heart, Lung, and Blood Institute	K99HL125728
National Cancer Institute	T32CA009206

Keywords

imaging
lanthanum
positron emission tomography
radiochemistry
radiopharmaceuticals

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10.1002/chem.201905202

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title = "Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications",

abstract = "We report the first targeted nuclear medicine application of the lanthanum radionuclides 132/135La. These isotopes represent a matched pair for diagnosis via the positron emissions of 132La and therapy mediated by the Auger electron emissions of 135La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides. The 18-membered macrocycle, macropa, bound 132/135La with better molar activity than DO3Apic under similar conditions. These chelators were conjugated to the prostate-specific membrane antigen (PSMA)-targeting agent DUPA to assess the use of radiolanthanum for in vivo imaging. The 132/135La-labeled targeted constructs showed high uptake in tumor xenografts expressing PSMA. This study validates the use of these radioactive lanthanum isotopes for imaging applications and motivates future work to assess the therapeutic effects of the Auger electron emissions of 135La.",

keywords = "imaging, lanthanum, positron emission tomography, radiochemistry, radiopharmaceuticals",

author = "Eduardo Aluicio-Sarduy and Thiele, {Nikki A.} and Martin, {Kirsten E.} and Vaughn, {Brett A.} and Justin Devaraj and Olson, {Aeli P.} and Barnhart, {Todd E.} and Wilson, {Justin J.} and Eszter Boros and Engle, {Jonathan W.}",

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year = "2020",

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doi = "10.1002/chem.201905202",

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AU - Devaraj, Justin

AU - Olson, Aeli P.

AU - Barnhart, Todd E.

AU - Wilson, Justin J.

AU - Boros, Eszter

AU - Engle, Jonathan W.

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N2 - We report the first targeted nuclear medicine application of the lanthanum radionuclides 132/135La. These isotopes represent a matched pair for diagnosis via the positron emissions of 132La and therapy mediated by the Auger electron emissions of 135La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides. The 18-membered macrocycle, macropa, bound 132/135La with better molar activity than DO3Apic under similar conditions. These chelators were conjugated to the prostate-specific membrane antigen (PSMA)-targeting agent DUPA to assess the use of radiolanthanum for in vivo imaging. The 132/135La-labeled targeted constructs showed high uptake in tumor xenografts expressing PSMA. This study validates the use of these radioactive lanthanum isotopes for imaging applications and motivates future work to assess the therapeutic effects of the Auger electron emissions of 135La.

AB - We report the first targeted nuclear medicine application of the lanthanum radionuclides 132/135La. These isotopes represent a matched pair for diagnosis via the positron emissions of 132La and therapy mediated by the Auger electron emissions of 135La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides. The 18-membered macrocycle, macropa, bound 132/135La with better molar activity than DO3Apic under similar conditions. These chelators were conjugated to the prostate-specific membrane antigen (PSMA)-targeting agent DUPA to assess the use of radiolanthanum for in vivo imaging. The 132/135La-labeled targeted constructs showed high uptake in tumor xenografts expressing PSMA. This study validates the use of these radioactive lanthanum isotopes for imaging applications and motivates future work to assess the therapeutic effects of the Auger electron emissions of 135La.

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Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications

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