Recurrent glioblastoma multiforme – targeted alpha therapy with 213Bi-DOTA-Substance P

Królicki, Leszek; Królicki, Bartosz; Morgenstern, Alfred; Kunikowska, J.; Koziara, Henryk; Jakuciński, Maciej; Apostolidis, C.; Bruchertseifer, Frank

doi:10.1016/s0167-8140(16)30032-9

Cited by 3 publications

(8 citation statements)

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“…A study comparing 213 Bi-DOTA-PESIN with 177 Lu-DOTA-PESIN demonstrated superior tumor-growth control and survival rates for the α-treated group . When labeled with 213 Bi, substance P has demonstrated improved median survival time for treatment of malignant primary brain tumors (Glioblastoma multiforme, GBM), compared to conventional treatment (25.2 vs 14.6 months) . Plasminogen activator inhibitor type 2 (PAI2) has been heavily investigated and shown promise with 213 Bi for treatment of breast, prostate, pancreatic, and ovarian cancer. − The most recent 213 Bi-PAI2 study was dosimetry based with aspirations of phase I clinical trials; however, over the past decade no such studies have been published.…”

Section: Bismuthmentioning

confidence: 99%

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

2018

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Radiometals possess an exceptional breadth of decay properties and have been applied to medicine with great success for several decades. The majority of current clinical use involves diagnostic procedures, which use either positron-emission tomography (PET) or single-photon imaging to detect anatomic abnormalities that are difficult to visualize using conventional imaging techniques (e.g., MRI and X-ray). The potential of therapeutic radiometals has more recently been realized and relies on ionizing radiation to induce irreversible DNA damage, resulting in cell death. In both cases, radiopharmaceutical development has been largely geared toward the field of oncology; thus, selective tumor targeting is often essential for efficacious drug use. To this end, the rational design of fourcomponent radiopharmaceuticals has become popularized. This Review introduces fundamental concepts of drug design and applications, with particular emphasis on bifunctional chelators (BFCs), which ensure secure consolidation of the radiometal and targeting vector and are integral for optimal drug performance. Also presented are detailed accounts of production, chelation chemistry, and biological use of selected main group and rare earth radiometals.

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Section: Bismuthmentioning

confidence: 99%

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

2018

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“…This will facilitate the selection of patients who might benefit from CXCR4-directed therapy. Another example is [ 131 I]-labeled anti-tenascin murine 81C6 mAb SPECT to assess the distribution of the radiolabeled mAb in brain parenchyma [93][94][95][96]. ($) radiopharmaceutical are grouped as in preclinical (P) and clinical (C) stages of development; chelating agents for radiometal complexation were not denoted in the names to improve clarity of presentation; (++) Fatty acid synthesis (acetate) and choline metabolism for choline; pivalic acid undergoes intracellular metabolism via the fatty acid oxidation pathway (an berrant lipid metabolite detection), (£) no trivial name available-UPAC: 7-chloro-N,N,5-trimethyl-4-oxo-3(6-[ 18 F]fluoropyridin-2-yl)-3,5-dihydro-4Hpyridazino [4,5-b]indole-1-acetamide, ( ## ) no names given -a small library of nonradioactive analogs were designed and synthesized based on the chemical structure of reported butyl-phenyl sulfonamide enzyme inhibitors, (*) currently in clinical translation, (ç) DNA-based oligonucleotide (aptamer), (°) RNA based oligonucleotide (aptamer), (**) protein-mimic cluster, (+) dual-imaging modality -investigatory (proof-of-concept), ( $$ ) expressed on glioma-associated macrophages and microglia, ( ǂ ) vectors: amino-acid (AA), antibody (Ab), antibody fragment (Abf), small biomolecule (SM), peptide (Pep), protein (Prot), oligonucleotide (ON).…”

Section: Selection Of the Appropriate Theranostic Pair For Individual...mentioning

confidence: 99%

“…Calculations have shown that as few as five high LET α-particle traversals through the cell nucleus are enough to kill a cell, whereas 10,000-20,000 low LET β-particles are needed to achieve the same biological effect [130]. In addition, TAT is also suggested as a facilitator to overcome tumoral resistance to chemotherapy and the effect of radiation independently to O6-methylguanine-DNA methyltransferase promoter methylation status; the most important predictor factor in TMZ treatment [93]. Of all known α-particle-emitting radionuclides, three: actinium-225, astatine-211 and bismuth-213 have received the most attention for TAT and RIT.…”

Section: α-Particlesmentioning

confidence: 99%

“…Generally, a combined treatment strategy is suggested to advance GB treatment efficacy aim to address the following challenges: i) the infiltrative character of the tumour beyond a safety margin makes it impossible to surgically resect all GB cells, ii) systemic chemotherapy reaches the cerebral compartment only to a limited extent and iii) hypoxia and an acidotic milieu of the intratumoral and peritumoral microenvironment reduce the efficacy of EBRT and chemotherapy. Additionally, tumour heterogeneity and the multiple pathways involved could lead to signalling redundancy [93]. Currently, TRT can be considered as a potent, additive treatment after the standard treatment for primary GB or as an auxiliary treatment when the tumour tissue seems to be radio-and/or chemoresistant.…”

Section: Selection Of a Combined Treatment Strategymentioning

confidence: 99%

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A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma

Bolcaen¹,

Kleynhans²,

Nair³

et al. 2021

Theranostics

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Despite numerous clinical trials and pre-clinical developments, the treatment of glioblastoma (GB) remains a challenge. The current survival rate of GB averages one year, even with an optimal standard of care. However, the future promises efficient patient-tailored treatments, including targeted radionuclide therapy (TRT). Advances in radiopharmaceutical development have unlocked the possibility to assess disease at the molecular level allowing individual diagnosis. This leads to the possibility of choosing a tailored, targeted approach for therapeutic modalities. Therapeutic modalities based on radiopharmaceuticals are an exciting development with great potential to promote a personalised approach to medicine. However, an effective targeted radionuclide therapy (TRT) for the treatment of GB entails caveats and requisites. This review provides an overview of existing nuclear imaging and TRT strategies for GB. A critical discussion of the optimal characteristics for new GB targeting therapeutic radiopharmaceuticals and clinical indications are provided. Considerations for target selection are discussed, i.e. specific presence of the target, expression level and pharmacological access to the target, with particular attention to blood-brain barrier crossing. An overview of the most promising radionuclides is given along with a validation of the relevant radiopharmaceuticals and theranostic agents (based on small molecules, peptides and monoclonal antibodies). Moreover, toxicity issues and safety pharmacology aspects will be presented, both in general and for the brain in particular.

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“…Novel targeted therapeutic approaches have been presented also for malignant brain tumours (Królicki et al) using 213 B-labeled DOTA-substance P [ 24 ]. The authors demonstrated that this approach is safe and well tolerated, resulting in PFS of 3.7 months.…”

Section: Oncology: Therapymentioning

confidence: 99%

Highlights lecture EANM 2015: the search for nuclear medicine’s superheroes

Buck

Decristoforo

2016

Eur J Nucl Med Mol Imaging

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The EANM 2015 Annual Congress, held from October 10th to 14th in Hamburg, Germany, was outstanding in many respects. With 5550 participants, this was by far the largest European congress concerning nuclear medicine. More than 1750 scientific presentations were submitted, with more than 250 abstracts from young scientists, indicating that the future success of our discipline is fuelled by a high number of young individuals becoming involved in a multitude of scientific activities. Significant improvements have been made in molecular imaging of cancer, particularly in prostate cancer. PSMA-directed PET/CT appears to become a new gold standard for staging and restaging purposes. Novel tumour specific compounds have shown their potential for target identification also in other solid neoplasms and further our understanding of tumour biology and heterogeneity. In addition, a variety of nuclear imaging techniques guiding surgical interventions have been introduced. A particular focus of the congress was put on targeted, radionuclide based therapies. Novel theranostic concepts addressing also tumour entities with high incidence rates such as prostate cancer, melanoma, and lymphoma, have shown effective anti-tumour activity. Strategies have been presented to improve further already established therapeutic regimens such as somatostatin receptor based radio receptor therapy for treating advanced neuroendocrine tumours. Significant contributions were presented also in the neurosciences track. An increasing number of target structures of high interest in neurology and psychiatry are now available for PET and SPECT imaging, facilitating specific imaging of different subtypes of dementia and movement disorders as well as neuroinflammation. Major contributions in the cardiovascular track focused on further optimization of cardiac perfusion imaging by reducing radiation exposure, reducing scanning time, and improving motion correction. Besides coronary artery disease, many contributions focused on cardiac inflammation, cardiac sarcoidosis, and specific imaging of large vessel vasculitis. The physics and instrumentation track included many highlights such as novel, high resolution scanners. The most noteworthy news and developments of this meeting were summarized in the highlights lecture. Only 55 scientific contributions were mentioned, and hence they represent only a brief summary, which is outlined in this article. For a more detailed view, all presentations can be accessed by the online version of the European Journal of Nuclear Medicine and Molecular Imaging (Volume 42, Supplement 1).

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Recurrent glioblastoma multiforme – targeted alpha therapy with 213Bi-DOTA-Substance P

Cited by 3 publications

References 0 publications

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma

Highlights lecture EANM 2015: the search for nuclear medicine’s superheroes

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