Comparison of novel PSMA-targeting [177Lu]Lu-P17-087 with its albumin binding derivative [177Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study

Li, Linlin; Wang, Jiarou; Wang, Guochang; Wang, Rongxi; Jin, Wenbin; Zang, Jie; Sui, Huimin; Jia, Chenhao; Jiang, Yuanyuan; Hong, Haiyan; Zhu, Lin; Alexoff, David; Ploessl, Karl; Kung, Hank F.; Zhu, Zhaohui

doi:10.1007/s00259-024-06721-x

Cited by 4 publications

(1 citation statement)

References 41 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Serving as a close analog to [ 68 Ga]Ga-PSMA-11, [ 68 Ga]Ga/[ 18 F]AlF-P16-093 presents itself as a promising PSMA-targeting PET imaging agent, currently undergoing clinical trials for the diagnosis and monitoring of prostate cancer patients. − Moreover, P19-065, P17-087 and P17-088, utilizing DOTAGA or DOTAGA 2 as the chelator, exhibit the capability to be labeled with Ga-68 and Lu-177 for prostate cancer therapy. Recent investigations reveal that [ 177 Lu]Lu-P17-087 and [ 177 Lu]Lu-P17-088 display favorable in vivo pharmacokinetics and therapeutic efficacy . Additionally, we have introduced an agent with dual targeting of bone and PSMA, [ 68 Ga]Ga/[ 177 Lu]Lu-P17-079 .…”

Section: Introductionmentioning

confidence: 99%

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

Luo,

Jin,

Wang

et al. 2024

J. Med. Chem.

Self Cite

View full text Add to dashboard Cite

Prostate-specific membrane antigen (PSMA) is an excellent target for cancer detection and therapy. Hypoxia is prevalent in solid tumors, and various nitroimidazole (NI) radioligands can be trapped inside hypoxic cells for diagnosis and therapy. To enhance tumor uptake and retention, we designed bivalent agents (compounds 1−8) incorporating a hypoxia-sensitive NI-moiety and a PSMA-targeting group. Ligands 1−8 were successfully prepared and labeled with 68 Ga or 177 Lu. Among them, [ 68 Ga]Ga-8 ([ 68 Ga]Ga-AAZTA-NI-PSMA-093) demonstrated significantly higher cellular accumulation under hypoxic conditions than under normoxic conditions, suggesting hypoxia-selective trapping by the introduction of NI group. PET/CT imaging at 60 min postinjection of [ 68 Ga]Ga-8 revealed high tumor uptake (SUV max : 10.68%ID/mL) in the tumor-bearing mice model. SPECT/CT imaging of [ 177 Lu]Lu-8 at 24 and 48 h postinjection demonstrated excellent accumulation and retention. Preliminary studies indicate that [ 68 Ga]Ga/[ 177 Lu]Lu-8 may be promising bivalent agents targeting hypoxia and PSMA binding for diagnosis and radiotherapy.

show abstract

Section: Introductionmentioning

confidence: 99%

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

Luo,

Jin,

Wang

et al. 2024

J. Med. Chem.

Self Cite

View full text Add to dashboard Cite

show abstract

Comparison of Radionuclide Drug Conjugates With Boron Neutron Capture Therapy: An Overview of Targeted Charged Particle Radiation Therapy

Zhang,

Coghi,

Ren

et al. 2024

Medicinal Research Reviews

View full text Add to dashboard Cite

Targeted charged alpha‐ and beta‐particle therapies are currently being used in clinical radiation treatments as newly developed methods for either killing or controlling tumor cell growth. The alpha particles can be generated either through a nuclear decay reaction or in situ by a nuclear fission reaction such as the boron neutron capture reaction. Different strategies have been employed to improve the selectivity and delivery of radiation dose to tumor cells based on the source of the clinically used alpha particles. As a result, the side effects of the treatment can be minimized. The increasing attention and research efforts on targeted alpha‐particle therapy have been fueled by exciting results of both academic research and clinical trials. It is highly anticipated that alpha‐particle therapy will improve the efficacy of treating malignant tumors. In this overview, we compare radionuclide drug conjugates (RDC) with boron neutron capture therapy (BNCT) to present recent developments in targeted alpha‐particle therapy.

show abstract

Safety, pharmacokinetics, and dosimetry of 177Lu-AB-3PRGD2 in patients with advanced integrin αvβ3-positive tumors: a first-in-human study

Sui,

Guo,

Liu

et al. 2024

Acta Pharmaceutica Sinica B

View full text Add to dashboard Cite

Comparison of novel PSMA-targeting [177Lu]Lu-P17-087 with its albumin binding derivative [177Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study

Cited by 4 publications

References 41 publications

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

Comparison of Radionuclide Drug Conjugates With Boron Neutron Capture Therapy: An Overview of Targeted Charged Particle Radiation Therapy

Safety, pharmacokinetics, and dosimetry of 177Lu-AB-3PRGD2 in patients with advanced integrin αvβ3-positive tumors: a first-in-human study

Contact Info

Product

Resources

About

Comparison of novel PSMA-targeting [177Lu]Lu-P17-087 with its albumin binding derivative [177Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study

Cited by 4 publications

References 41 publications

68Ga/177Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

68Ga/177Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

Comparison of Radionuclide Drug Conjugates With Boron Neutron Capture Therapy: An Overview of Targeted Charged Particle Radiation Therapy

Safety, pharmacokinetics, and dosimetry of 177Lu-AB-3PRGD2 in patients with advanced integrin αvβ3-positive tumors: a first-in-human study

Contact Info

Product

Resources

About

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer

⁶⁸Ga/¹⁷⁷Lu-Labeled Bivalent Agents for Targeting Hypoxia and PSMA-Binding in Prostate Cancer