Clinical Perspectives of Theranostics

Okamoto, Susumu; Shiga, Tohru; Tamaki, Nagara

doi:10.3390/molecules26082232

Cited by 23 publications

(17 citation statements)

References 66 publications

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“…Also from a theranostic point of view, PK modelling approaches could improve dosimetry research. Though an important assumption in theranostics is that the diagnostic and therapeutic counterpart behave alike, retrospective studies showed varying degrees of concordance between pre-therapeutic and therapeutic accumulation of the radiopharmaceuticals [53][54][55][56][57][58][59]. The discrepancies between pre-therapeutic and therapeutic biodistribution are attributed to factors like targeting peptide, peptide dosing, use of co-medication and/or chosen imaging time-points, which can be accounted for in these models.…”

Section: Population Dosimetrymentioning

confidence: 99%

Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review

Siebinga¹,

Veen²,

Stokkel³

et al. 2022

Theranostics

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Rationale: Physiologically based pharmacokinetic (PBPK) and population pharmacokinetic (PK) modelling approaches are widely accepted in non-radiopharmaceutical drug development and research, while there is no major role for these approaches in radiopharmaceutical development yet. In this review, a literature search was performed to specify different research purposes and questions that have previously been answered using both PBPK and population PK modelling for radiopharmaceuticals. Methods: The literature search was performed using the databases PubMed and Embase. Wide search terms included radiopharmaceutical, tracer, radioactivity, physiologically based pharmacokinetic model, PBPK, population pharmacokinetic model and nonlinear mixed-effects model. Results: Eight articles and twenty articles were included for this review based on this literature search for population PK modelling and PBPK modelling, respectively. Included population PK analyses showed to have an added value to develop predictive models for a population and to describe individual variability sources. Main purposes of PBPK models appeared related to optimizing treatment (planning), or more specifically: to find the optimal combination of peptide amount and radioactivity, to optimize treatment planning by reducing the number of measurements, to individualize treatment, to get insights in differences between pre-therapeutic and therapeutic scans or to understand inter-patient differences. Other main research subjects were regarding radiopharmaceutical comparisons, selecting ligands based on their peptide characteristics and gaining a better understanding of drug-drug interactions. Conclusions: The use of PK modelling approaches in radiopharmaceutical research remains scarce, but can be expanded to obtain a better understanding of PK and whole-body distribution of radiopharmaceuticals in general. PK modelling of radiopharmaceuticals has great potential for the nearby future and could contribute to the evolving research of radiopharmaceuticals.

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Section: Population Dosimetrymentioning

confidence: 99%

Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review

Siebinga¹,

Veen²,

Stokkel³

et al. 2022

Theranostics

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“…This therapy concept involving α-particle emitters has been well-reviewed in the literature [68,69]. It is also important to note that α-particle emitters have already made a significant impact in theranostics in instances where the condition treated has become refractory to β-emitter therapy [70]. In the search for valuable cancer therapies, there is a wide range of research committed to develop nano-sized theranostics; in particular within nuclear medicine the field of nano-theranostics has not yet gained momentum.…”

Section: The Way Forward?mentioning

confidence: 99%

Obstacles and Recommendations for Clinical Translation of Nanoparticle System-Based Targeted Alpha-Particle Therapy

2021

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The rationale for application of nanotechnology in targeted alpha therapy (TAT) is sound. However, the translational strategy requires attention. Formulation of TAT in nanoparticulate drug delivery systems has the potential to resolve many of the issues currently experienced. As α-particle emitters are more cytotoxic compared to beta-minus-emitting agents, the results of poor biodistribution are more dangerous. Formulation in nanotechnology is also suggested to be the ideal solution for containing the recoil daughters emitted by actinium-225, radium-223, and thorium-227. Nanoparticle-based TAT is likely to increase stability, enhance radiation dosimetry profiles, and increase therapeutic efficacy. Unfortunately, nanoparticles have their own unique barriers towards clinical translation. A major obstacle is accumulation in critical organs such as the spleen, liver, and lungs. Furthermore, inflammation, necrosis, reactive oxidative species, and apoptosis are key mechanisms through which nanoparticle-mediated toxicity takes place. It is important at this stage of the technology’s readiness level that focus is shifted to clinical translation. The relative scarcity of α-particle emitters also contributes to slow-moving research in the field of TAT nanotechnology. This review describes approaches and solutions which may overcome obstacles impeding nanoparticle-based TAT and enhance clinical translation. In addition, an in-depth discussion of relevant issues and a view on technical and regulatory barriers are presented.

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“…Theranostics is a term in the medical field to define the combination of therapeutic and diagnostic techniques by a suitable pharmaceutical agent [ 1 ]. It is an effort to improve therapeutic interventions after imaging is performed to find the target entity of the disease [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker

et al. 2022

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Therapeutic radiopharmaceuticals have been researched extensively in the last decade as a result of the growing research interest in personalized medicine to improve diagnostic accuracy and intensify intensive therapy while limiting side effects. Radiometal-based drugs are of substantial interest because of their greater versatility for clinical translation compared to non-metal radionuclides. This paper comprehensively discusses various components commonly used as chemical scaffolds to build radiopharmaceutical agents, i.e., radionuclides, pharmacokinetic-modifying linkers, and chelators, whose characteristics are explained and can be used as a guide for the researcher.

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Clinical Perspectives of Theranostics

Cited by 23 publications

References 66 publications

Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review

Current use and future potential of (physiologically based) pharmacokinetic modelling of radiopharmaceuticals: a review

Obstacles and Recommendations for Clinical Translation of Nanoparticle System-Based Targeted Alpha-Particle Therapy

The Chemical Scaffold of Theranostic Radiopharmaceuticals: Radionuclide, Bifunctional Chelator, and Pharmacokinetics Modifying Linker

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