4.7 Article

Preclinical Evaluation of a Lead Specific Chelator (PSC) Conjugated to Radiopeptides for 203Pb and 212Pb-Based Theranostics

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Oncology

Mathematical Modeling of In Vivo Alpha Particle Generators and Chelator Stability

Nouran R. R. Zaid et al.

Summary: A mathematical model was developed to describe the kinetics of Pb-212-labeled pharmaceuticals and its radioactive daughters. The simulation revealed that alpha emissions contributed significantly to the total released energy, and the Bi-212-DOTAM complexes had a certain dissociation during retention. The contributions of different chelators to the energy released by free radionuclides were varied.

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS (2023)

Article Radiology, Nuclear Medicine & Medical Imaging

Targeted a-Emitter Therapy with 212Pb-DOTAMTATE for the Treatment of Metastatic SSTR-Expressing Neuroendocrine Tumors: First-in-Humans Dose-Escalation Clinical Trial

Ebrahim S. Delpassand et al.

Summary: The targeted α-therapy with Pb-212-DOTAMTATE showed good tolerability and promising preliminary efficacy in treating patients with somatostatin receptor-positive NETs.

JOURNAL OF NUCLEAR MEDICINE (2022)

Article Biochemistry & Molecular Biology

Dosimetry of [212Pb]VMT01, a MC1R-Targeted Alpha Therapeutic Compound, and Effect of Free 208Tl on Tissue Absorbed Doses

Kelly D. Orcutt et al.

Summary: The goal of this study is to estimate the human dosimetry for [Pb-212]VMT01 and the impact of free Tl-208 in the injectate on human tissue absorbed doses. The results indicate that the dose-limiting tissues for [Pb-212]VMT01 are the red marrow and the kidneys, while absorbed doses from free Tl-208 in the injectate have a minimal increase.

MOLECULES (2022)

Article Radiology, Nuclear Medicine & Medical Imaging

Predictive factors of tumor sink effect: Insights from 177Lu-Prostate-specific membrane antigen therapy

Murat Tuncel et al.

Summary: The study investigated predictive factors of the tumor sink effect in patients receiving Lu-177-PSMA therapy for progressive metastatic castration-resistant prostate cancer (mCRPC). It found that Ga-68-PSMA TLPI, pre-therapy PSA, and PSA velocity were predictors of TSE, which can lead to increased tumoral doses while sparing healthy organs and potentially increasing therapeutic efficacy in clinical trials.

ANNALS OF NUCLEAR MEDICINE (2021)

Article Pharmacology & Pharmacy

A Physiologically Based Pharmacokinetic Model for In Vivo Alpha Particle Generators Targeting Neuroendocrine Tumors in Mice

Nouran R. R. Zaid et al.

Summary: The study developed a murine whole-body PBPK model for Pb-212-SSTA, finding that alpha-PRRT based on Pb-212-SSTA results in lower absorbed doses in non-target tissues compared to Bi-212-SSTA. The model demonstrates that the majority of energy release in the kidneys occurs in the glomeruli and proximal tubules.

PHARMACEUTICS (2021)

Article Oncology

Targeted Alpha-Particle Radiotherapy and Immune Checkpoint Inhibitors Induces Cooperative Inhibition on Tumor Growth of Malignant Melanoma

Mengshi Li et al.

Summary: The study demonstrated the feasibility of delivering alpha-particle radiation to murine melanoma tumors using a radiolabeled peptide that targets the melanocortin 1 receptor. The combination of targeted alpha-particle radionuclide therapy and immune checkpoint inhibitors showed significant anti-tumor cooperation in preclinical models of melanoma, mediated by induction of tumor-specific immunity.

CANCERS (2021)

Article Biochemistry & Molecular Biology

Clinically Applicable Cyclotron-Produced Gallium-68 Gives High-Yield Radiolabeling of DOTA-Based Tracers

Emma Jussing et al.

Summary: By adding ascorbate in the purification process, the level of metal impurities in (GaCl3)-Ga-68 was significantly lowered, allowing for high-yield radiolabeling of clinically relevant DOTA-based tracers. The resulting Ga-68 eluate could be used for GMP-compliant syntheses, yielding radiochemically pure and stable products.

BIOMOLECULES (2021)

Article Chemistry, Inorganic & Nuclear

Getting a lead on Pb2+-amide chelators for 203/212Pb radiopharmaceuticals

Aidan Ingham et al.

Summary: Amide-based chelators DTPAm, EGTAm, and ampam were synthesized and studied for their coordination properties with [Pb-nat/203]Pb2+ ions using H-1 NMR spectroscopy and X-ray diffraction. Results showed that DTPAm exhibited higher stability and activity, making it a promising candidate for [Pb-203/212]Pb2+-based radiopharmaceutical applications, while EGTAm and ampam showed lower performance and were deemed unsuitable for similar applications.

DALTON TRANSACTIONS (2021)

Review Chemistry, Medicinal

Peptide Receptor Radionuclide Therapy: Looking Back, Looking Forward

Danny Feijtel et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Molecular Bismuth Cations: Assessment of Soft Lewis Acidity

Jacqueline Ramler et al.

CHEMISTRY-A EUROPEAN JOURNAL (2020)

Review Biotechnology & Applied Microbiology

Radiopharmaceutical therapy in cancer: clinical advances and challenges

George Sgouros et al.

NATURE REVIEWS DRUG DISCOVERY (2020)

Review Biochemistry & Molecular Biology

203/212Pb Theranostic Radiopharmaceuticals for Image-guided Radionuclide Therapy for Cancer

Mengshi Li et al.

CURRENT MEDICINAL CHEMISTRY (2020)

Article Physics, Nuclear

Nuclear Data Sheets for A=212

K. Auranen et al.

NUCLEAR DATA SHEETS (2020)

Article Chemistry, Inorganic & Nuclear

An octadentate bis(semicarbazone) macrocycle: a potential chelator for lead and bismuth radiopharmaceuticals

Jaclyn L. Lange et al.

DALTON TRANSACTIONS (2020)

Article Medicine, Research & Experimental

Evaluation of a Novel Pb-203-Labeled Lactam-Cyclized Alpha-Melanocyte-Stimulating Hormone Peptide for Melanoma Targeting

Jianquan Yang et al.

MOLECULAR PHARMACEUTICS (2019)

Article Radiology, Nuclear Medicine & Medical Imaging

Development and dosimetry of 203Pb/212Pb-labelled PSMA ligands: bringing the lead into PSMA-targeted alpha therapy?

Jose Carlos dos Santos et al.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2019)

Article Radiology, Nuclear Medicine & Medical Imaging

Relevant tumor sink effect in prostate cancer patients receiving 177Lu-PSMA-617 radioligand therapy

Christian Filss et al.

NUKLEARMEDIZIN-NUCLEAR MEDICINE (2018)

Article Oncology

Peptide Receptor Radionuclide Therapy in the Treatment of Neuroendocrine Tumors

Dik J. Kwekkeboom et al.

HEMATOLOGY-ONCOLOGY CLINICS OF NORTH AMERICA (2016)

Article Radiology, Nuclear Medicine & Medical Imaging

225Ac-PSMA-617 for PSMA-Targeted a-Radiation Therapy of Metastatic Castration-Resistant Prostate Cancer

Clemens Kratochwil et al.

JOURNAL OF NUCLEAR MEDICINE (2016)

Article Oncology

Molecular Pathways: Targeted α-Particle Radiation Therapy

Kwamena E. Baidoo et al.

CLINICAL CANCER RESEARCH (2013)

Article Chemistry, Analytical

Search of ligands suitable for 212Pb/212Bi in vivo generators

Barbara Bartos et al.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY (2013)

Article Endocrinology & Metabolism

SSTR2 is the functionally dominant somatostatin receptor in human pancreatic β- and α-cells

Balrik Kailey et al.

AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM (2012)

Article Nuclear Science & Technology

212Pb/212Bi GENERATOR FOR NUCLEAR MEDICINE

P. P. Boldyrev et al.

ATOMIC ENERGY (2012)

Article Radiology, Nuclear Medicine & Medical Imaging

Comparison of receptor affinity of Sc-nat-DOTA-TATE versus Ga-nat-DOTA-TATE

Eftychia Koumarianou et al.

NUCLEAR MEDICINE REVIEW (2011)

Review Radiology, Nuclear Medicine & Medical Imaging

MIRD Pamphlet No. 22 (Abridged): Radiobiology and Dosimetry of α-Particle Emitters for Targeted Radionuclide Therapy

George Sgouros et al.

JOURNAL OF NUCLEAR MEDICINE (2010)

Review Pharmacology & Pharmacy

Alpha-particles for targeted therapy

George Sgouros

ADVANCED DRUG DELIVERY REVIEWS (2008)

Article Radiology, Nuclear Medicine & Medical Imaging

203Pb-labeled α-melanocyte-stimulating hormone peptide as an imaging probe for melanoma detection

Yubin Miao et al.

JOURNAL OF NUCLEAR MEDICINE (2008)

Review Physics, Nuclear

Nuclear data sheets for A=208

M. J. Martin

NUCLEAR DATA SHEETS (2007)

Article Radiology, Nuclear Medicine & Medical Imaging

Pretargeted radioimmunotherapy in tumored mice using an in vivo 212Pb/212Bi generator

FM Su et al.

NUCLEAR MEDICINE AND BIOLOGY (2005)

Article Oncology

Melanoma therapy via peptide-targeted α-radiation

YB Miao et al.

CLINICAL CANCER RESEARCH (2005)

Review Pharmacology & Pharmacy

Phage display-derived peptides as a therapeutic alternatives to antibodies

RC Ladner et al.

DRUG DISCOVERY TODAY (2004)