225Ac- and 213Bi-Substance P Analogues for Glioma Therapy

Królicki, Leszek; Kunikowska, Jolanta; Bruchertseifer, Frank; Koziara, Henryk; Królicki, Bartosz; Jakuciński, Maciej; Pawlak, Dariusz; Rola, Rafał; Morgenstern, Alfred; Rosiak, Elżbieta; Merlo, Adrian

doi:10.1053/j.semnuclmed.2019.11.004

Cited by 41 publications

(51 citation statements)

References 67 publications

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“…Even if 213 Bi-DOTA-SP emerged as a new option of treatment of gliomas, the short half-life of 213 Bi can be a limit in the homogenous distribution in large tumors. That is in that conditions that longer half-life radioisotope such as 225 Ac can be of interest [ 178 ].…”

Section: Bismuth-213mentioning

confidence: 99%

Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

et al. 2021

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Among all existing radionuclides, only a few are of interest for therapeutic applications and more specifically for targeted alpha therapy (TAT). From this selection, actinium-225, astatine-211, bismuth-212, bismuth-213, lead-212, radium-223, terbium-149 and thorium-227 are considered as the most suitable. Despite common general features, they all have their own physical characteristics that make them singular and so promising for TAT. These radionuclides were largely studied over the last two decades, leading to a better knowledge of their production process and chemical behavior, allowing for an increasing number of biological evaluations. The aim of this review is to summarize the main properties of these eight chosen radionuclides. An overview from their availability to the resulting clinical studies, by way of chemical design and preclinical studies is discussed.

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Section: Bismuth-213mentioning

confidence: 99%

Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

et al. 2021

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“…CED has been applied in the clinic and was proved to be a safe and effective drug delivery method for GB with limited systemic toxicity [ 510 ]. Most RIT strategies for malignant gliomas were administered locally into the postsurgical cavity or intratumorally and the first results on the local administration of [ 213 Bi]Bi-substance P and [ 225 Ac]Ac-substance P are promising [ 511 , 512 , 513 , 514 ]. Overall, GB management would greatly benefit from the introduction of TRT using TKI-based radiopharmaceuticals.…”

Section: Selection and Radiolabeling Of New Tkis For Trt Of Gbmentioning

confidence: 99%

“…Finally, we would like to point out that besides these RTKs that contain intrinsic enzyme activity, there are numerous other plasma membrane receptors that can influence downstream intracellular signaling pathways which play a major role in GB persistence and progression. These include the folate receptors and the NK-1 receptor that lead to development of radiolabeled folate-chelate conjugates and radiolabeled substance-P [ 511 , 514 , 515 ]. The advantage of TKIs is that many are designed to be multi-targeted, affecting multiple signaling pathways concomitantly.…”

Section: Selection and Radiolabeling Of New Tkis For Trt Of Gbmentioning

confidence: 99%

Novel Receptor Tyrosine Kinase Pathway Inhibitors for Targeted Radionuclide Therapy of Glioblastoma

et al. 2021

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Glioblastoma (GB) remains the most fatal brain tumor characterized by a high infiltration rate and treatment resistance. Overexpression and/or mutation of receptor tyrosine kinases is common in GB, which subsequently leads to the activation of many downstream pathways that have a critical impact on tumor progression and therapy resistance. Therefore, receptor tyrosine kinase inhibitors (RTKIs) have been investigated to improve the dismal prognosis of GB in an effort to evolve into a personalized targeted therapy strategy with a better treatment outcome. Numerous RTKIs have been approved in the clinic and several radiopharmaceuticals are part of (pre)clinical trials as a non-invasive method to identify patients who could benefit from RTKI. The latter opens up the scope for theranostic applications. In this review, the present status of RTKIs for the treatment, nuclear imaging and targeted radionuclide therapy of GB is presented. The focus will be on seven tyrosine kinase receptors, based on their central role in GB: EGFR, VEGFR, MET, PDGFR, FGFR, Eph receptor and IGF1R. Finally, by way of analyzing structural and physiological characteristics of the TKIs with promising clinical trial results, four small molecule RTKIs were selected based on their potential to become new therapeutic GB radiopharmaceuticals.

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“…Expansion of this series reported on results of therapy in 17 patients [154]. More recently the same approach has been utilized for therapy with the alpha emitters 213 Bi [155] and 225 Ac [156](Fig. 5), which have been monitored using PET imaging by co-injecting 68 Ga labeled peptide.…”

Section: Peptides and Small Moleculesmentioning

confidence: 99%

Imaging and treatment of brain tumors through molecular targeting: Recent clinical advances

Zaccagna

Grist

Quartuccio

et al. 2021

European Journal of Radiology

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Molecular imaging techniques have rapidly progressed over recent decades providing unprecedented in vivo characterization of metabolic pathways and molecular biomarkers. Many of these new techniques have been successfully applied in the field of neuro-oncological imaging to probe tumor biology. Targeting specific signaling or metabolic pathways could help to address several unmet clinical needs that hamper the management of patients with brain tumors. This review aims to provide an overview of the recent advances in brain tumor imaging using molecular targeting with positron emission tomography and magnetic resonance imaging, as well as the role in patient management and possible therapeutic implications.

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225Ac- and 213Bi-Substance P Analogues for Glioma Therapy

Cited by 41 publications

References 67 publications

Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”

Novel Receptor Tyrosine Kinase Pathway Inhibitors for Targeted Radionuclide Therapy of Glioblastoma

Imaging and treatment of brain tumors through molecular targeting: Recent clinical advances

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