Current status and future perspective of radiopharmaceuticals in China

Ji, Hu; Li, Hongyu; Sui, Yanying; Du, Jianjun

doi:10.1007/s00259-021-05615-6

Cited by 17 publications

(12 citation statements)

References 79 publications

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“…In recent years, the radiopharmaceutical industry has gradually attracted the attention of investors also thanks to specific government strategic plans, which provide a roadmap in driving forward the promotion of the research, development, production, and clinical application of radiopharmaceuticals in the country. China is expected to be one of the most important markets in the near future offering renewed opportunities for investors in Nuclear Medicine both in established and emerging technologies …”

Section: Resultsmentioning

confidence: 99%

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Riondato

Rigamonti²,

Martini

et al. 2023

J. Med. Chem.

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Technetium-99m is the workhorse of diagnostic nuclear medicine. The aim of the work is to analyze the technetium-99m patents since 2000 to photograph its innovation. QUESTEL’s ORBIT Intelligence system was used for the collection of technetium inventions disclosed in patents and patent applications in more than 96 countries in the period 2000–2022; 2768 patent documents were analyzed. Patent counting and analysis have shown that SPECT imaging using technetium-99m radiopharmaceuticals is still robust. The introduction of new technetium-99m radiopharmaceuticals into clinical routine goes beyond successful trials. In eastern economies, such as China and other emerging markets, patent applications are on the rise, while those in developed western countries are stagnating, with some exceptions for the United States. But despite the difficulties, academic and industrial research on these tracers remains essential for the development of nuclear medicine.

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Section: Resultsmentioning

confidence: 99%

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Riondato

Rigamonti²,

Martini

et al. 2023

J. Med. Chem.

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“…7−10 18 F, a radioisotope of 19 F, has favorable nuclide properties for PET, i.e., a moderate halflife (about 110 min), a high β + decay ratio (97%), and a relatively low maximum positron energy (634 keV). 11 Due to the excellent properties of fluorinated drugs and the universal use of medical cyclotrons in medical institutions, 12,13 the development of simple, mild, and efficient 18 F-labeling methods has become an important goal of radiopharmaceutical chemistry research. 14,15 18 F-Labeling methods can be classified into electrophilic fluorination, nucleophilic fluorination, metal-F coordination, and 18 F/ 19 F isotope exchange.…”

Section: Introductionmentioning

confidence: 99%

“…The introduction of one or more F atoms or F-containing groups into drug molecules is a common strategy to improve their stability and bioavailability. − 18 F, a radioisotope of 19 F, has favorable nuclide properties for PET, i.e., a moderate half-life (about 110 min), a high β + decay ratio (97%), and a relatively low maximum positron energy (634 keV) . Due to the excellent properties of fluorinated drugs and the universal use of medical cyclotrons in medical institutions, , the development of simple, mild, and efficient 18 F-labeling methods has become an important goal of radiopharmaceutical chemistry research. , …”

Section: Introductionmentioning

confidence: 99%

Isotope Exchange-Based ¹⁸F-Labeling Methods

Wang

Mou

et al. 2023

Bioconjugate Chem.

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18 F-Labeling methods for the preparation of 18 F-labeled molecular probes can be classified into electrophilic fluorination, nucleophilic fluorination, metal-F coordination, and 18 F/ 19 F isotope exchange. Isotope exchange-based 18 F-labeling methods demonstrate mild conditions featuring water resistance and facile high-performance liquid chromatography-free purification in direct 18 F-labeling of substrates. This paper systematically reviews isotope exchange-based 18 F-labeling methods sorted by the adjacent atom bonding with F, i.e., carbon and noncarbon atoms (Si, B, P, S, Ga, Fe, etc.). The respective isotope exchange mechanism, radiolabeling condition, radiochemical yield, molar activity, and stability of the 18 F-product are mainly discussed for each isotope exchange-based 18 F-labeling method as well as the cuttingedge application of the corresponding 18 F-labeled molecular probes.

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“…10 Currently, worldwide, especially in developing countries, the number of SPECT scanners is still far greater than that of PET scanners. 11,12 Convenient sources and low prices of nuclides have greatly promoted the development of technetium-99m radiopharmaceuticals. Quinolones, a large class of antibiotics, can specifically bind DNA topoisomerase of bacteria.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Benefiting from the success of 99 Mo/ 99m Tc generator commercialization, technetium-99m has developed into the most widely used SPECT nuclide in clinical practice . Currently, worldwide, especially in developing countries, the number of SPECT scanners is still far greater than that of PET scanners. , Convenient sources and low prices of nuclides have greatly promoted the development of technetium-99m radiopharmaceuticals.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Bioevaluation of Novel Technetium-99m-Labeled Complexes with Norfloxacin HYNIC Derivatives for Bacterial Infection Imaging

et al. 2022

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To seek a novel 99m Tc-labeled quinolone derivative for bacterial infection SPECT imaging that aims to lower nontarget organ uptake, a novel norfloxacin 6-hydrazinoicotinamide (HYNIC) derivative (HYNICNF) was designed and synthesized. It was radiolabeled with different coligands, such as tricine, trisodium triphenylphosphine-3,3′,3″-trisulfonate (TPPTS), sodium triphenylphosphine-3-monosulfonate (TPPMS), and ethylenediamine-N,N′-diacetic acid (EDDA), to obtain three 99m Tclabeled norfloxacin HYNIC complexes, namely, [ 99m Tc]Tc-tricine-TPPTS-HYNICNF, [ 99m Tc]Tc-tricine-TPPMS-HYNICNF, and [ 99m Tc]Tc-EDDA-HYNICNF. These complexes were purified (RCP > 95%) and evaluated in vitro and in vivo for targeting bacteria. All three complexes are hydrophilic, maintain good stability, and specifically bind Staphylococcus aureus in vitro. The biodistribution in mice with bacterial infection demonstrated that [ 99m Tc]Tc-EDDA-HYNICNF showed a higher abscess uptake and lower nontarget organ uptake and was able to distinguish bacterial infection and sterile inflammation. Single photon emission computed tomography (SPECT) image study in bacterial infection mice showed there was a visible accumulation in the infection site, suggesting that [ 99m Tc]Tc-EDDA-HYNICNF is a potential radiotracer for bacterial infection imaging.

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Current status and future perspective of radiopharmaceuticals in China

Cited by 17 publications

References 79 publications

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Isotope Exchange-Based ¹⁸F-Labeling Methods

Synthesis and Bioevaluation of Novel Technetium-99m-Labeled Complexes with Norfloxacin HYNIC Derivatives for Bacterial Infection Imaging

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Current status and future perspective of radiopharmaceuticals in China

Cited by 17 publications

References 79 publications

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Oldie but Goodie: Is Technetium-99m Still a Treasure Trove of Innovation for Medicine? A Patents Analysis (2000–2022)

Isotope Exchange-Based 18F-Labeling Methods

Synthesis and Bioevaluation of Novel Technetium-99m-Labeled Complexes with Norfloxacin HYNIC Derivatives for Bacterial Infection Imaging

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Isotope Exchange-Based ¹⁸F-Labeling Methods