Bench to bedside development of GMP grade Rhenium-188-HEDP, a radiopharmaceutical for targeted treatment of painful bone metastases

Heine, Rob ter; Lange, Rogier; Breukels, Oscar; Bloemendal, Haiko J.; Rummenie, Rob G; Wakker, Antoinette M; Graaf, Hilly de; Beekman, Freek J.; Westerlaken, Monique M. L. van der; Malingré, Mirte M.; Wielders, Jos P.M.; Berg, Leo van den; Hendrikse, N. Harry; Klerk, John M. H. de

doi:10.1016/j.ijpharm.2014.01.034

Cited by 26 publications

(9 citation statements)

References 21 publications

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“…Alpha-and beta-emitting radioisotopes such as 223 Ra and 188 Re are already used in the clinic for metastatic castration-resistant prostate cancer. Safety studies show that treatment with these radioisotopes is associated with minimal adverse events [64,65]. Nonetheless, it is important to consider survival time, age, physical and emotional wellbeing and alternative treatment options.…”

Section: Discussionmentioning

confidence: 99%

Treating infections with ionizing radiation: a historical perspective and emerging techniques

Dijk

Lemans

Hoogendoorn

et al. 2020

Antimicrob Resist Infect Control

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Background: Widespread use and misuse of antibiotics have led to a dramatic increase in the emergence of antibiotic resistant bacteria, while the discovery and development of new antibiotics is declining. This has made certain implant-associated infections such as periprosthetic joint infections, where a biofilm is formed, very difficult to treat. Alternative treatment modalities are needed to treat these types of infections in the future. One candidate that has been used extensively in the past, is the use of ionizing radiation. This review aims to provide a historical overview and future perspective of radiation therapy in infectious diseases with a focus on orthopedic infections. Methods: A systematic search strategy was designed to select studies that used radiation as treatment for bacterial or fungal infections. A total of 216 potentially relevant full-text publications were independently reviewed, of which 182 focused on external radiation and 34 on internal radiation. Due to the large number of studies, several topics were chosen. The main advantages, disadvantages, limitations, and implications of radiation treatment for infections were discussed. Results: In the pre-antibiotic era, high mortality rates were seen in different infections such as pneumonia, gas gangrene and otitis media. In some cases, external radiation therapy decreased the mortality significantly but longterm follow-up of the patients was often not performed so long term radiation effects, as well as potential increased risk of malignancies could not be investigated. Internal radiation using alpha and beta emitting radionuclides show great promise in treating fungal and bacterial infections when combined with selective targeting through antibodies, thus minimizing possible collateral damage to healthy tissue. Conclusion: The novel prospects of radiation treatment strategies against planktonic and biofilm-related microbial infections seem feasible and are worth investigating further. However, potential risks involving radiation treatment must be considered in each individual patient.

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Section: Discussionmentioning

confidence: 99%

Treating infections with ionizing radiation: a historical perspective and emerging techniques

Dijk

Lemans

Hoogendoorn

et al. 2020

Antimicrob Resist Infect Control

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“…All of them pointed out that the addition of carrier was crucial. A GMP grade kit for the preparation of 188 Re-HEDP has recently been described (119) and a standard procedure following the ICH Q8 guideline, and investigating the critical step parameters, has been reported by the same team (118).…”

Section: Re-labeled Small Moleculesmentioning

confidence: 99%

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

et al. 2019

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Rhenium-188 ( 188 Re) is a high energy beta-emitting radioisotope with a short 16.9 h physical half-life, which has been shown to be a very attractive candidate for use in therapeutic nuclear medicine. The high beta emission has an average energy of 784 keV and a maximum energy of 2.12 MeV, sufficient to penetrate and destroy targeted abnormal tissues. In addition, the low-abundant gamma emission of 155 keV (15%) is efficient for imaging and for dosimetric calculations. These key characteristics identify 188 Re as an important therapeutic radioisotope for routine clinical use. Moreover, the highly reproducible on-demand availability of 188 Re from the 188 W/ 188 Re generator system is an important feature and permits installation in hospital-based or central radiopharmacies for cost-effective availability of no-carrier-added (NCA) 188 Re. Rhenium-188 and technetium-99 m exhibit similar chemical properties and represent a “theranostic pair.” Thus, preparation and targeting of 188 Re agents for therapy is similar to imaging agents prepared with 99m Tc, the most commonly used diagnostic radionuclide. Over the last three decades, radiopharmaceuticals based on 188 Re-labeled small molecules, including peptides, antibodies, Lipiodol and particulates have been reported. The successful application of these 188 Re-labeled therapeutic radiopharmaceuticals has been reported in multiple early phase clinical trials for the management of various primary tumors, bone metastasis, rheumatoid arthritis, and endocoronary interventions. This article reviews the use of 188 Re-radiopharmaceuticals which have been investigated in patients for cancer treatment, demonstrating that 188 Re represents a cost effective alternative for routine clinical use in comparison to more expensive and/or less readily available therapeutic radioisotopes.

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“…For the ease and dependable routine preparation of radiopharmaceuticals the use of sterile/pyrogen-free substrate/radiolabeling mixtures ("kits") offers many advantages for quality, dependable and easy preparation. In the context of this issue of IJNMR, several useful "kits" have been recently developed for preparation of 188 Re-labeled radiopharmaceuticals, and include kits for radiopharmacy preparation of HEDP for bone pain palliation [72][73][74][75][76], and Lipiodol analogues (DEDC, Re-SSS) for treatment of inoperable hepatic carcinoma [77][78]. It would be expected that further development of new "kits" will be reported if the expected expanded clinical use of other attractive 188 Re radiopharmaceuticals progresses.…”

Section: Re-targeting Agentsmentioning

confidence: 99%

Continued Availability of the Tungsten-188/Rhenium-188 Generator to Enhance Therapeutic Utility of 188Re

Knapp¹

2017

Int. J. Nucl. Medi. Res.

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Rhenium-188 (188 Re) is a high energy beta-emitting radioisotope of widespread interest for use in nuclear medicine, oncology and other therapeutic applications. High energy beta emission (16.9 hour half-life) with Emax 2.12 MeV and gamma emission at 155 keV (15 %) are key factors for effective therapy and imaging for tissue kinetics and dosimetry evaluation. Moreover, on-demand availability of 188 Re in a highly reproducible manner from the 188 W/ 188 Re generator system is an important capability for installation in a hospital-based or a central radiopharmacy for cost effective availability of no-carrier-added (NCA) 188 Re. Because of the long 69.7 day half-life of the 188 W generator parent, the use of well-established post 188 Re elution specific volume concentration technology allow generators to have a useful/predictable operational shelf-life of a few months. This paper provides a holistic review of the development, availability and use of the 188 W/ 188 Re generator prototypes.

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Bench to bedside development of GMP grade Rhenium-188-HEDP, a radiopharmaceutical for targeted treatment of painful bone metastases

Cited by 26 publications

References 21 publications

Treating infections with ionizing radiation: a historical perspective and emerging techniques

Treating infections with ionizing radiation: a historical perspective and emerging techniques

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

Continued Availability of the Tungsten-188/Rhenium-188 Generator to Enhance Therapeutic Utility of 188Re

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