Options to meet the future global demand of radionuclides for radionuclide therapy

Das, Tapas; Pillai, M.R.A.

doi:10.1016/j.nucmedbio.2012.09.007

Cited by 77 publications

(60 citation statements)

References 93 publications

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“…Alternatively, 89 Sr can be produced using 89 Y(n,p) 89 Sr nuclear reaction, but the cross-section of this reaction with thermal neutrons is even lower than the 88 Sr(n,γ) 89 Sr reaction (0.0002044 versus 0.058 barns). Consequently, the costs of 89 Sr-based bone pain palliation therapies are expected to remain high (Das and Pillai, 2013). In addition to the high production costs and low reactions yields, the specific activity of the formed 89 Sr is very low when obtained by direct production.…”

Section: Iib Strontium-89mentioning

confidence: 99%

“…117m Sn is produced either by neutron activation using enriched 116 Sn target, via the 116 Sn(n,γ) 117m Sn nuclear reaction or by inelastic neutron scattering on enriched 117 Sn, 117 Sn(n,n',γ) 117m Sn (Das and Pillai, 2013;Maslov et al, 2011). However, owing to the poor crosssection of both these reactions and the need for a very high flux reactor and highly enriched targets that are essential to produce sufficient quantities of 117m Sn, large-scale production of this radionuclide is not practical.…”

Section: Iid Tin-117mmentioning

confidence: 99%

“…Therefore, radiotherapy agents labelled with 177m Sn would have low myelotoxicity (Das and Pillai, 2013). Moreover, the gamma emission of 117m Sn is in the ideal range for scintigraphic interrogation, thus allowing for acquisition of images for dosimetry estimates, as well as, for treatment response monitoring.…”

Section: Iid Tin-117mmentioning

confidence: 99%

“…A notable example is the treatment of hyperthyroidism and thyroid cancer using Na 131 I. Since then, a wide variety of radiolabeled agents has been used clinically for treatment of different types of diseases, but only a limited number of these preparations have obtained regulatory approval for routine clinical use in patients and are commercially available (Das and Pillai, 2013). Examples of diseases that have been treated by nuclear medicine therapy are: thyroid carcinoma, hyperthyroidism, metastatic bone pain, polycythemia rubra vera, neuroendocrine tumors (NETs), liver metastases, lymphoma and neuroblastoma.…”

Section: Introductionmentioning

confidence: 99%

“…Among these, treatment of thyroid cancer with 131 I is the most widely used radionuclide-targeted therapy. The second most widely used application is for bone pain palliation in the context of metastatic cancer (Das and Pillai, 2013).…”

Section: Introductionmentioning

confidence: 99%

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Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Liberal

Tavares

2016

Applied Radiation and Isotopes

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Purpose: The present review article aims to provide an overview of the available radionuclides for palliative treatment of bone metastases beyond 89 Sr and 153 Sm. In addition, it aims to review and summarize the clinical outcomes associated with the palliative treatment of bone metastases using different radiopharmaceuticals. Materials and Methods: A literature search was conducted on Science Direct and PubMed databases (1990 -2015). The following search terms were combined in order to obtain relevant results: "bone", "metastases", "palliative", "care", "therapy", "treatment", "radiotherapy", "review", "radiopharmaceutical", "phosphorus-32", "strontium-89", "yttrium-90", "tin-117m", "samarium-153", "holmium-166", "thulium-170", "lutetium-177", "rhenium-186", "rhenium-188" and "radium-223". Studies were included if they provided information regarding the clinical outcomes. Results and Conclusions: A comparative analysis of the measured therapeutic response of different radiopharmaceuticals, based on previously published data, suggests that there is a lack of substantial differences in palliative efficacy among radiopharmaceuticals. However, when the comparative analysis adds factors such as patient's life expectancy, radionuclides' physical characteristics (e.g. tissue penetration range and half-life) and health economics to guide the rational selection of a radiopharmaceutical for palliative treatment of bone metastases, 177 Lu and 188 Re-labeled radiopharmaceuticals appear to be the most suitable radiopharmaceuticals for treatment of small and medium/large size bone lesions, respectively.

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Section: Iib Strontium-89mentioning

confidence: 99%

Section: Iid Tin-117mmentioning

confidence: 99%

Section: Iid Tin-117mmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Liberal

Tavares

2016

Applied Radiation and Isotopes

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Synthesis and evaluation of [¹⁷⁷Lu]Lu‐labeled porphyrin loaded PAMAM dendrimer: Impact on tumor uptake and pharmacokinetics

Kumar

Guleria

et al. 2022

Drug Development Research

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The objective of the present work is to evaluate the ability of the radiolabeled PAMAM dendrimers (polyamidoamine) towards facilitating the delivery of an in‐house synthesized porphyrin derivative in the tumorous lesions to evaluate their candidature for possible application in endo‐radionuclide therapy. For this, PAMAM particles were conjugated with a porphyrin derivative namely, 5,10,15,20‐tetrakis‐(4‐carboxymethyleneoxyphenyl)porphyrin (STAP), synthesized in‐house following a two‐step reaction. The average number of porphyrin molecules loaded per PAMAM particle was evaluated using ultraviolet‐visible spectrophotometry and was found to be approximately 2. STAP conjugated PAMAM particles were further conjugated with p‐NCS‐benzyl‐DOTA (subsequently referred as DOTA) to facilitate radiolabeling with 177Lu. On an average, two p‐NCS‐benzyl‐DOTA molecules were observed to be attached per PAMAM‐STAP particle. DOTA‐PAMAM‐STAP conjugate was radiolabeled with 177Lu with a final radiochemical purity of >95%, which was determined by paper chromatography using two different mobile phases viz. 0.1 M sodium citrate buffer (pH 5.0) and 10 mM DTPA. Biological behavior of [177Lu]Lu‐DOTA‐PAMAM‐STAP conjugate was investigated in fibrosarcoma bearing Swiss mice model wherein accumulation of radiolabeled particles was observed in liver, GIT, spleen, and kidneys at 3 h post‐administration. However, accumulated activity exhibited rapid clearance from majority of the organs at 24 h post‐administration. [177Lu]Lu‐DOTA‐PAMAM‐STAP conjugate exhibited an appreciable uptake in tumor mass [6.09 ± 1.22 percentage injected activity/organ (% IA/organ)] at 3 h post‐administration (p.i.) which was found to reduce to 1.05 ± 0.13 % IA/organ at 24 h post‐administration. The results obtained in biodistribution studies were further corroborated through scintigraphic imaging performed in the same animal model. Despite of an appreciable accumulation in tumor mass, the lower retention of the [177Lu]Lu‐DOTA‐PAMAM‐STAP conjugate therein, at longer time point (24 h p.i.) may limit its possible potential as a radio‐therapeutic agent and indicates towards need for further structural manoeuvring to attain favorable in vivo performance.

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⁹⁰Y/¹⁷⁷Lu‐labelled Cetuximab immunoconjugates: radiochemistry optimization to clinical dose formulation

Chakravarty

Chakraborty

Sarma

et al. 2016

Labelled Comp Radiopharmac

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Radiolabelled monoclonal antibodies (mAbs) are increasingly being utilized in cancer theranostics, which is a significant move toward tailored treatment for individual patients. Cetuximab is a recombinant, human-mouse chimeric IgG1 mAb that binds to the epidermal growth factor receptor with high affinity. We have optimized a protocol for formulation of clinically relevant doses (~2.22 GBq) of (90) Y-labelled Cetuximab and (177) Lu-labelled Cetuximab by conjugation of the mAb with a suitable bifunctional chelator, N-[(R)-2-amino-3-(paraisothiocyanato-phenyl)propyl]-trans-(S,S)-cyclohexane-1,2-diamine-N,N,N',N″,N″-pentaacetic acid (CHX-A″-DTPA). The radioimmunoconjugates demonstrated reasonably high specific activity (1.26 ± 0.27 GBq/mg for (90) Y-CHX-A″-DTPA-Cetuximab and 1.14 ± 0.15 GBq/mg for (177) Lu-CHX-A″-DTPA-Cetuximab), high radiochemical purity (>95%) and appreciable in vitro stability under physiological conditions. Preliminary biodistribution studies with both (90) Y-CHX-A″-DTPA-Cetuximab and (177) Lu-CHX-A″-DTPA-Cetuximab in Swiss mice bearing fibrosarcoma tumours demonstrated significant tumour uptake at 24-h post-injection (p.i.) (~16%ID/g) with good tumour-to-background contrast. The results of the biodistribution studies were further corroborated by ex vivo Cerenkov luminescence imaging after administration of (90) Y-CHX-A″-DTPA-Cetuximab in tumour-bearing mice. The tumour uptake at 24 h p.i. was significantly reduced with excess unlabelled Cetuximab, suggesting that the uptake was receptor mediated. The results of this study hold promise, and this strategy should be further explored for clinical translation.

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Options to meet the future global demand of radionuclides for radionuclide therapy

Cited by 77 publications

References 93 publications

Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Synthesis and evaluation of [¹⁷⁷Lu]Lu‐labeled porphyrin loaded PAMAM dendrimer: Impact on tumor uptake and pharmacokinetics

⁹⁰Y/¹⁷⁷Lu‐labelled Cetuximab immunoconjugates: radiochemistry optimization to clinical dose formulation

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Options to meet the future global demand of radionuclides for radionuclide therapy

Cited by 77 publications

References 93 publications

Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Palliative treatment of metastatic bone pain with radiopharmaceuticals: A perspective beyond Strontium-89 and Samarium-153

Synthesis and evaluation of [177Lu]Lu‐labeled porphyrin loaded PAMAM dendrimer: Impact on tumor uptake and pharmacokinetics

90Y/177Lu‐labelled Cetuximab immunoconjugates: radiochemistry optimization to clinical dose formulation

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Product

Resources

About

Synthesis and evaluation of [¹⁷⁷Lu]Lu‐labeled porphyrin loaded PAMAM dendrimer: Impact on tumor uptake and pharmacokinetics

⁹⁰Y/¹⁷⁷Lu‐labelled Cetuximab immunoconjugates: radiochemistry optimization to clinical dose formulation