Review
Chemistry, Multidisciplinary
Feize Li, Yuanyou Yang, Jiali Liao, Ning Liu
Summary: Astatine-211 (At-211) is a promising alpha-emitter for targeted-alpha therapy (TAT) in various malignancies, due to its high linear energy transfer and short tissue range. In the past two decades, significant progress has been made in At-211-related radiopharmaceutical research, providing important insights for tumor radiotherapy and other radiopharmaceutical studies.
CHINESE CHEMICAL LETTERS
(2022)
Article
Pharmacology & Pharmacy
Xuhao Huang, Kazuko Kaneda-Nakashima, Yuichiro Kadonaga, Kazuya Kabayama, Atsushi Shimoyama, Kazuhiro Ooe, Hiroki Kato, Atsushi Toyoshima, Atsushi Shinohara, Hiromitsu Haba, Yang Wang, Koichi Fukase
Summary: This study demonstrates the significant anti-tumor effect of 5 nm At-211-AuNPs@mPEG in inhibiting tumor growth in a pancreatic cancer model. AuNPs serve as satisfactory carriers for At-211 delivery, offering a simple and efficient synthesis process and high stability.
Article
Radiology, Nuclear Medicine & Medical Imaging
Erik Leidermark, Andreas Hallqvist, Lars Jacobsson, Per Karlsson, Erik Holmberg, Tom Back, Mia Johansson, Sture Lindegren, Stig Palm, Per Albertsson
Summary: Intraperitoneal At-211-based targeted alpha-therapy (TAT) shows promise as adjuvant therapy for ovarian cancer. However, long-term risks need to be estimated to determine whether the treatment is justified.
JOURNAL OF NUCLEAR MEDICINE
(2023)
Article
Biotechnology & Applied Microbiology
Hiroki Kato, Xuhao Huang, Yuichiro Kadonaga, Daisuke Katayama, Kazuhiro Ooe, Atsushi Shimoyama, Kazuya Kabayama, Atsushi Toyoshima, Atsushi Shinohara, Jun Hatazawa, Koichi Fukase
Summary: At-211-AuNP-S-mPEG showed cytotoxicity to tumor cells and localized in the tumor after intratumoral administration, without spreading to systemic organs, leading to strong suppression of tumor growth.
JOURNAL OF NANOBIOTECHNOLOGY
(2021)
Review
Medicine, General & Internal
Per Albertsson, Tom Baeck, Karin Bergmark, Andreas Hallqvist, Mia Johansson, Emma Aneheim, Sture Lindegren, Chiara Timperanza, Knut Smerud, Stig Palm
Summary: Astatine-211 is a top candidate for targeted alpha therapy (TAT) due to its physical properties. In this article, we summarize the results of completed clinical trials, provide an overview of ongoing trials, and discuss future prospects.
FRONTIERS IN MEDICINE
(2023)
Review
Biochemistry & Molecular Biology
Albert Jang, Ayse T. Kendi, Geoffrey B. Johnson, Thorvardur R. Halfdanarson, Oliver Sartor
Summary: Radiopharmaceuticals are rapidly developing as a field, with targeted beta and alpha emitters being investigated for oncologic indications. Clinical trials are currently underway for conjugated/chelated alpha emitters, with multiple diseases being targeted in phase I trials and a phase III trial in neuroendocrine cancers. Challenges remain in terms of supply chains, understanding administered dose and absorbed dose relationships, and potential long-term effects of alpha emitters.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tadashi Watabe, Kazuko Kaneda-Nakashima, Yoshifumi Shirakami, Yuichiro Kadonaga, Kazuhiro Ooe, Yang Wang, Hiromitsu Haba, Atsushi Toyoshima, Jens Cardinale, Frederik L. Giesel, Noriyuki Tomiyama, Koichi Fukase
Summary: This study evaluated the treatment effect of At-211-labeled PSMA compounds in mouse xenograft models. The results showed that TAT using [At-211]PSMA5 resulted in excellent tumor growth suppression with minimal side effects, suggesting it as a potential new treatment for metastatic CRPC.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Hiroaki Echigo, Kenji Mishiro, Masayuki Munekane, Takeshi Fuchigami, Kohshin Washiyama, Kazuhiro Takahashi, Yoji Kitamura, Hiroshi Wakabayashi, Seigo Kinuya, Kazuma Ogawa
Summary: We developed probes for multiradionuclides radiotheranostics using RGD peptide and an albumin binding moiety. The use of 4-(4-astatophenyl)-butyric acid as the albumin binding moiety improved the therapeutic effects of targeted alpha therapy. [At-211]5 showed higher tumor accumulation and retention compared to other probes.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Nanoscience & Nanotechnology
Yang Liu, Zhengyuan Zhou, Yutian Feng, Xiao-Guang Zhao, Ganesan Vaidyanathan, Michael R. Zalutsky, Tuan Vo-Dinh
Summary: Developing an innovative At-211 nanoplatform with high radiolabeling efficiency and low in vivo deastatination for targeted alpha-particle therapy (TAT) to treat cancer showed promising results. The new platform demonstrated high labeling efficiency, excellent in vivo stability, and significant tumor growth inhibition.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2021)
Review
Pharmacology & Pharmacy
Bryce J. B. Nelson, Jan D. Andersson, Frank Wuest
Summary: This review discusses the therapeutic advantages of targeted alpha particle therapy, the properties and radiochemistry of common alpha-emitters, production techniques, ongoing and completed clinical trials, and future outlook of TAT.
Article
Medicine, Research & Experimental
Weihao Liu, Huan Ma, Ranxi Liang, Xijian Chen, Hongyan Li, Tu Lan, Jijun Yang, Jiali Liao, Zhi Qin, Yuanyou Yang, Ning Liu, Feize Li
Summary: Targeted radionuclide therapy based on alpha-emitters is important in cancer treatment. This study proposes a new vector for At-211 radiolabeling and demonstrates its effectiveness in inhibiting tumor growth and promoting cell apoptosis without significant toxicity to normal organs.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Inorganic & Nuclear
Weihao Liu, Yu Tang, Huan Ma, Feize Li, Yingjiang Hu, Yuanyou Yang, Jijun Yang, Jiali Liao, Ning Liu
Summary: The study demonstrates that At-211 labeled VP2 fusion peptide exhibits more effective cytotoxicity against malignant epithelial tumors in vitro and in vivo, leading to significant tumor growth inhibition and prolonged survival in mice.
Article
Biochemistry & Molecular Biology
Ayaka Aso, Hinako Nabetani, Yoshifumi Matsuura, Yuichiro Kadonaga, Yoshifumi Shirakami, Tadashi Watabe, Taku Yoshiya, Masayoshi Mochizuki, Kazuhiro Ooe, Atsuko Kawakami, Naoya Jinno, Atsushi Toyoshima, Hiromitsu Haba, Yang Wang, Jens Cardinale, Frederik Lars Giesel, Atsushi Shimoyama, Kazuko Kaneda-Nakashima, Koichi Fukase
Summary: In this study, four novel At-211-FAPI(s) with PEG linkers were designed and synthesized, and their FAP selectivity and uptake were tested. The results showed that PEG linkers had equivalent antitumor effects to PIP linkers, indicating that PEG linkers can serve as alternatives to PIP linkers.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Engineering, Chemical
Tianzhen Ye, Yilin Qin, Weihao Liu, Lingting Xia, Jiali Liao, Jijun Yang, Tu Lan, Yuanyou Yang, Ning Liu, Feize Li
Summary: This study presents a new solid-phase extraction (SPE) separation strategy for recovering astatine-211 (At-211) from irradiated bismuth targets. The use of acyl-resin as a functional material showed good retention of At-211 and low binding affinity to metal impurities. The SPE separation process can be completed within 20 minutes, providing At-211 product with high radionuclidic purity and low metal impurities. This method has potential applications in medical-scale separations.
SEPARATION AND PURIFICATION TECHNOLOGY
(2024)
Review
Pharmacology & Pharmacy
Romain Eychenne, Michel Cherel, Ferid Haddad, Francois Guerard, Jean-Francois Gestin
Summary: This review summarizes the main properties of eight selected radionuclides, including their production process, chemical behavior, and biological evaluations, discussing the entire process from their availability to clinical studies.
Article
Oncology
Anna E. Nordenskjold, Helena. Fohlin, Lars G. Arnesson, Zakaria Einbeigi, Erik Holmberg, Per Albertsson, Per Karlsson
Article
Radiology, Nuclear Medicine & Medical Imaging
Andreas Hallqvist, Karin Bergmark, Tom Back, Hakan Andersson, Pernilla Dahm-Kahler, Mia Johansson, Sture Lindegren, Holger Jensen, Lars Jacobsson, Ragnar Hultborn, Stig Palm, Per Albertsson
JOURNAL OF NUCLEAR MEDICINE
(2019)
Article
Biology
R. Hultborn, P. Albertsson, S. Ottosson, E. Warnhammar, A. Palm, S. Palm, K. Elmroth
RADIATION RESEARCH
(2019)
Article
Medicine, Research & Experimental
Yana Dekempeneer, Tom Back, Emma Aneheim, Holger Jensen, Janik Puttemans, Catarina Xavier, Marleen Keyaerts, Stig Palm, Per Albertsson, Tony Lahoutte, Vicky Caveliers, Sture Lindegren, Matthias D'Huyvetter
MOLECULAR PHARMACEUTICS
(2019)
Article
Radiology, Nuclear Medicine & Medical Imaging
Calvin N. Leung, Brian S. Canter, Didier Rajon, Tom A. Back, J. Christopher Fritton, Edouard Azzam, Roger W. Howell
JOURNAL OF NUCLEAR MEDICINE
(2020)
Article
Radiology, Nuclear Medicine & Medical Imaging
Tom A. Back, Karin Jennbacken, Malin Hagberg Thulin, Sture Lindegren, Holger Jensen, Tove Olafsen, Paul J. Yazaki, Stig Palm, Per Albertsson, Jan-Erik Damber, Anna M. Wu, Karin Welen
Article
Oncology
Stig Palm, Tom Back, Emma Aneheim, Andreas Hallqvist, Ragnar Hultborn, Lars Jacobsson, Holger Jensen, Sture Lindegren, Per Albertsson
Summary: The study aimed to evaluate the biodistribution and therapeutic effect of 211At-farletuzumab in vitro and in vivo, showing a 6 to 10-fold increase in antitumor efficacy compared to control groups. This observation suggests the potential for further clinical testing of intraperitoneal therapy with 211At-farletuzumab.
TRANSLATIONAL ONCOLOGY
(2021)
Article
Oncology
C. Chamalidou, H. Fohlin, P. Albertsson, L. -G. Arnesson, Z. Einbeigi, E. Holmberg, A. Nordenskjold, B. Nordenskjold, P. Karlsson, B. Linderholm
Summary: The study found that patients with invasive lobular carcinoma (ILC) had higher survival rates in the first five years after surgery compared to invasive ductal carcinoma (IDC), but in the 10-15 years after surgery, patients with ILC had a higher excess mortality rate ratio than those with IDC. After 20 years post-surgery, the relative survival rates for ILC and IDC were similar.
Article
Oncology
Charlotte Palmqvist, Josefine Persson, Per Albertsson, Pernilla Dahm-Kahler, Mia Johansson
Summary: This study evaluates the cost of illness of ovarian cancer in a population-based cohort. The results show that indirect costs constitute a large part of the cost of illness over the six-year follow-up period. With changes in treatment approaches and improved treatment outcomes, the societal cost may decrease.
Article
Oncology
Charlotte Palmqvist, Christian Staf, Constantina Mateoiu, Mia Johansson, Per Albertsson, Pernilla Dahm-Kahler
GYNECOLOGIC ONCOLOGY
(2020)