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Special Issue "Recent Advances in Radiopharmaceutics (Volume II)"

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School of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan
Interests: PET; SPECT; multimodality; imaging analysis; pharmacokinetics
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Dear Colleagues,

The development of radiopharmaceuticals is important for diagnosis and/or radionuclide therapy in nuclear medicine with positron emission tomography (PET) and single-photon emission computed tomography (SPECT). It also has translational potential from preclinical study to clinical in oncology, neurodegenerative diseases, cardiovascular diseases, etc., for personalized medicine. Integrative imaging and therapy, in combination with other modalities, such as magnetic resonance imaging, ultrasonography, near-infrared imaging, etc., may move personalized medicine further. In addition, advances in PET and SPECT scanners emphasize the usefulness of radiopharmaceuticals.

This Special Issue focuses on the synthesis and evaluation of new radiopharmaceuticals, other applications of radiopharmaceuticals for clinical use, and the combination of radionuclides with other modalities. Novel PET and SPECT machines are also a target. However, the areas of interest are not limited to these keywords.

Dr. Masato Kobayashi
Guest Editor

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Keywords

PET
SPECT
radiopharmaceutical
multimodality
imaging
biofunction
pharmacokinetics
imaging scanner

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Research

Open AccessArticle

[¹¹¹In]In/[¹⁷⁷Lu]Lu-AAZTA⁵-LM4 SST₂R-Antagonists in Cancer Theranostics: From Preclinical Testing to First Patient Results

Berthold A. Nock

Panagiotis Kanellopoulos

and

Pharmaceutics 2023, 15(3), 776; https://doi.org/10.3390/pharmaceutics15030776 - 26 Feb 2023

Cited by 1 | Viewed by 774

Abstract

Aiming to expand the application of the SST₂R-antagonist LM4 (DPhe-c[DCys-4Pal-DAph(Cbm)-Lys-Thr-Cys]-DTyr-NH₂) beyond [⁶⁸Ga]Ga-DATA^5m-LM4 PET/CT (DATA^5m, (6-pentanoic acid)-6-(amino)methy-1,4-diazepinetriacetate), we now introduce AAZTA⁵-LM4 (AAZTA⁵, 1,4-bis(carboxymethyl)-6-[bis(carboxymethyl)]amino-6-[pentanoic-acid]perhydro-1,4-diazepine), allowing for the convenient coordination of trivalent radiometals of clinical interest, such as In-111 (for SPECT/CT) or Lu-177 (for radionuclide therapy). After labeling, the preclinical profiles of [¹¹¹In]In-AAZTA⁵-LM4 and [¹⁷⁷Lu]Lu-AAZTA⁵-LM4 were compared in HEK293-SST₂R cells and double HEK293-SST₂R/wtHEK293 tumor-bearing mice using [¹¹¹In]In-DOTA-LM3 and [¹⁷⁷Lu]Lu-DOTA-LM3 as references. The biodistribution of [¹⁷⁷Lu]Lu-AAZTA⁵-LM4 was additionally studied for the first time in a NET patient. Both [¹¹¹In]In-AAZTA⁵-LM4 and [¹⁷⁷Lu]Lu-AAZTA⁵-LM4 displayed high and selective targeting of the HEK293-SST₂R tumors in mice and fast background clearance via the kidneys and the urinary system. This pattern was reproduced for [¹⁷⁷Lu]Lu-AAZTA⁵-LM4 in the patient according to SPECT/CT results in a monitoring time span of 4–72 h pi. In view of the above, we may conclude that [¹⁷⁷Lu]Lu-AAZTA⁵-LM4 shows promise as a therapeutic radiopharmaceutical candidate for SST₂R-expressing human NETs, based on previous [⁶⁸Ga]Ga-DATA^5m-LM4 PET/CT, but further studies are needed to fully assess its clinical value. Furthermore, [¹¹¹In]In-AAZTA⁵-LM4 SPECT/CT may represent a legitimate alternative diagnostic option in cases where PET/CT is not available. Full article

(This article belongs to the Special Issue Recent Advances in Radiopharmaceutics (Volume II))

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Open AccessArticle

Biological Distribution after Oral Administration of Radioiodine-Labeled Acetaminophen to Estimate Gastrointestinal Absorption Function via OATPs, OATs, and/or MRPs

and

Pharmaceutics 2023, 15(2), 497; https://doi.org/10.3390/pharmaceutics15020497 - 02 Feb 2023

Viewed by 708

Abstract

We evaluated the whole-body distribution of orally-administered radioiodine-125 labeled acetaminophen (¹²⁵I-AP) to estimate gastrointestinal absorption of anionic drugs. ¹²⁵I-AP was added to human embryonic kidney (HEK)293 and Flp293 cells expressing human organic anion transporting polypeptide (OATP)1B1/3, OATP2B1, organic anion transporter (OAT)1/2/3, or carnitine/organic cation transporter (OCTN)2, with and without bromosulfalein (OATP and multidrug resistance-associated protein (MRP) inhibitor) and probenecid (OAT and MRP inhibitor). The biological distribution in mice was determined by oral administration of ¹²⁵I-AP with and without bromosulfalein and by intravenous administration of ¹²⁵I-AP. The uptake of ¹²⁵I-AP was significantly higher in HEK293/OATP1B1, OATP1B3, OATP2B1, OAT1, and OAT2 cells than that in mock cells. Bromosulfalein and probenecid inhibited OATP- and OAT-mediated uptake, respectively. Moreover, ¹²⁵I-AP was easily excreted in the urine when administered intravenously. The accumulation of ¹²⁵I-AP was significantly lower in the blood and urinary bladder of mice receiving oral administration of both ¹²⁵I-AP and bromosulfalein than those receiving only ¹²⁵I-AP, but significantly higher in the small intestine due to inhibition of OATPs and/or MRPs. This study indicates that whole-body distribution after oral ¹²⁵I-AP administration can be used to estimate gastrointestinal absorption in the small intestine via OATPs, OATs, and/or MRPs by measuring radioactivity in the urinary bladder. Full article

(This article belongs to the Special Issue Recent Advances in Radiopharmaceutics (Volume II))

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Special Issue "Recent Advances in Radiopharmaceutics (Volume II)"

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