Advances in precision oncology: targeted thorium-227 conjugates as a new modality in targeted alpha therapy

UB Hagemann, K Wickstroem, S Hammer… - Cancer Biotherapy & …, 2020 - liebertpub.com
Targeted α therapy (TAT) offers the potential for the targeted delivery of potent α-particle-
emitting radionuclides that emit high linear energy transfer radiation. This leads to a densely …

Preclinical efficacy of a PSMA-targeted thorium-227 conjugate (PSMA-TTC), a targeted alpha therapy for prostate cancer

S Hammer, UB Hagemann, S Zitzmann-Kolbe… - Clinical Cancer …, 2020 - AACR
Purpose: Prostate-specific membrane antigen (PSMA) is an attractive target for radionuclide
therapy of metastatic castration-resistant prostate cancer (mCRPC). PSMA-targeted alpha …

Mesothelin-targeted thorium-227 conjugate (MSLN-TTC): preclinical evaluation of a new targeted alpha therapy for mesothelin-positive cancers

UB Hagemann, C Ellingsen, J Schuhmacher… - Clinical Cancer …, 2019 - AACR
Abstract Purpose: Targeted thorium-227 conjugates (TTC) represent a new class of
molecules for targeted alpha therapy (TAT). Covalent attachment of a 3, 2-HOPO chelator to …

In Vitro and In Vivo Efficacy of a Novel CD33-Targeted Thorium-227 Conjugate for the Treatment of Acute Myeloid Leukemia

UB Hagemann, K Wickstroem, E Wang, AO Shea… - Molecular cancer …, 2016 - AACR
The clinical efficacy of the first approved alpha pharmaceutical, Xofigo (radium-223
dichloride, 223RaCl2), has stimulated significant interest in the development of new alpha …

[HTML][HTML] Immunostimulatory effects of targeted thorium-227 conjugates as single agent and in combination with anti-PD-L1 therapy

P Lejeune, V Cruciani, A Berg-Larsen… - … for Immunotherapy of …, 2021 - ncbi.nlm.nih.gov
Background Targeted thorium-227 conjugates (TTCs) are an emerging class of targeted
alpha therapies (TATs). Their unique mode of action (MoA) is the induction of difficult-to …

[HTML][HTML] An efficient chelator for complexation of thorium-227

T Ramdahl, HT Bonge-Hansen, OB Ryan… - Bioorganic & Medicinal …, 2016 - Elsevier
We present the synthesis and characterization of a highly efficient thorium chelator, derived
from the octadentate hydroxypyridinone class of compounds. The chelator forms extremely …

[HTML][HTML] Targeted alpha therapy using a novel CD70 targeted thorium-227 conjugate in in vitro and in vivo models of renal cell carcinoma

UB Hagemann, D Mihaylova, SR Uran, J Borrebaek… - Oncotarget, 2017 - ncbi.nlm.nih.gov
The cell surface receptor CD70 has been previously reported as a promising target for B-cell
lymphomas and several solid cancers including renal cell carcinoma. We describe herein …

Solution thermodynamics and kinetics of metal complexation with a hydroxypyridinone chelator designed for thorium-227 targeted alpha therapy

GJP Deblonde, TD Lohrey, CH Booth… - Inorganic …, 2018 - ACS Publications
The solution chemistry of a chelator developed for 227Th targeted alpha therapy was
probed. The compound of interest is an octadentate ligand comprising four N-methyl-3 …

Synergistic effect of a mesothelin-targeted 227Th conjugate in combination with DNA damage response inhibitors in ovarian cancer xenograft models

K Wickstroem, UB Hagemann, V Cruciani… - Journal of Nuclear …, 2019 - Soc Nuclear Med
Targeted 227Th conjugates (TTCs) represent a new class of therapeutic
radiopharmaceuticals for targeted α-therapy. They comprise the α-emitter 227Th complexed …

In Vitro and In Vivo Comparison of 3,2-HOPO Versus Deferoxamine-Based Chelation of Zirconium-89 to the Antimesothelin Antibody Anetumab

J Roy, EM Jagoda, F Basuli, O Vasalatiy… - Cancer Biotherapy & …, 2021 - liebertpub.com
Introduction:[227Th] Th-3, 2-HOPO-MSLN-mAb, a mesothelin (MSLN)-targeted thorium-227
therapeutic conjugate, is currently in phase I clinical trial; however, direct PET imaging using …