Radiotracers to Address Unmet Clinical Needs in Cardiovascular Imaging, Part 2: Inflammation, Fibrosis, Thrombosis, Calcification, and Amyloidosis Imaging

Stendahl, John C.; Kwan, Jennifer M.; Pucar, Darko; Sadeghi, Mehran M.

doi:10.2967/jnumed.121.263507

Cited by 14 publications

(12 citation statements)

References 85 publications

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“…These include neuronal signaling, fibrosis, inflammation, amyloidosis, metabolic substrate utilization, and coronary artery plaques. These agents have great potential to address many clinical needs [ 35 , 38 ••, 39 – 41 ].…”

Section: New Pet Radiopharmaceuticals For Cardiac Studiesmentioning

confidence: 99%

Regulatory Agencies and PET/CT Imaging in the Clinic

Herscovitch

2022

Curr Cardiol Rep

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Purpose of Review The regulatory steps necessary to bring new PET radiopharmaceuticals to the clinic will be reviewed. The US Food and Drug Administration (FDA) provides approval to manufacture and use diagnostic radiopharmaceuticals, including those for cardiovascular PET/CT. Medicare not only provides insurance reimbursement for imaging procedures for its beneficiaries but also sets an example for third-party insurers to cover these procedures. Recent Findings FDA provides extensive guidance for performing studies to obtain the safety and efficacy data needed to approve PET radiopharmaceuticals, and the pace of approval has recently increased. There also has been considerable progress in insurance coverage for PET by Medicare. Several promising agents for cardiovascular PET imaging are in the development pipeline. Challenges remain, however, including low levels of reimbursement and the application of appropriate use criteria for imaging procedures. Summary It is important for cardiologists to understand the regulatory steps involved in translating PET radiopharmaceuticals to the clinic. Recent progress in both FDA approvals and Medicare coverage should facilitate the clinical use of new PET agents for molecular imaging of the heart.

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Section: New Pet Radiopharmaceuticals For Cardiac Studiesmentioning

confidence: 99%

Regulatory Agencies and PET/CT Imaging in the Clinic

Herscovitch

2022

Curr Cardiol Rep

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“…1 As a noninvasive imaging modality, positron emission tomography (PET) plays an important role in precision medicine given its unparalleled advantages in the identification of molecular targets and the visualization of biological processes. 2,3 The value of PET is also embodied in the ability to assess the in vivo distribution and pharmacokinetics of medicine by labeling appropriate positron-emitting nuclides. 4 18 F-fluorodeoxyglucose ( 18 F-FDG) is the most widely used radiotracer for PET imaging today; however, it has been hampered by well-described limitations (e.g., a lack of specificity) when applied to precision medicine.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Precision medicine is becoming a widely accepted guide to the action in the medical field, and its realization depends upon accuracy in the recognition of different targets . As a non-invasive imaging modality, positron emission tomography (PET) plays an important role in precision medicine given its unparalleled advantages in the identification of molecular targets and the visualization of biological processes. , The value of PET is also embodied in the ability to assess the in vivo distribution and pharmacokinetics of medicine by labeling appropriate positron-emitting nuclides …”

Section: Introductionmentioning

confidence: 99%

Exploration of ⁶⁸Ga-DOTA-MAL as a Versatile Vehicle for Facile Labeling of a Variety of Thiol-Containing Bioactive Molecules

Cheng

et al. 2023

ACS Omega

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Efficient and site-specific radiolabeling reactions are essential in molecular probe synthesis. Thus, selecting an effective method for radiolabeling that does not affect bioactivity of the molecule is critical. Varieties of bifunctional chelating agents provide a solution in this matter. As a chemo-specific chelator, maleimido-mono-amide-DOTA (DOTA-Mal) holds significant potential for 68Ga labeling of bioactive molecules; it can react specifically with free sulfhydryl groups under mild conditions. Compared with amino and carboxylic acid groups, free sulfhydryl groups are relatively less common in most biomolecules and can serve as site-specific radiolabeling targets. Labeling of 68Ga usually employs a two-step labeling strategy; first, chelators are conjugated to the biomolecules, which is followed by radiolabeling. However, the bioactivity of biomolecules may be affected by harsh labeling conditions. In this study, three 68Ga-labeled bioactive molecules, namely, 68Ga-DOTA-RGD, 68Ga-DOTA-FA, and 68Ga-DOTA-BSA, were prepared using a novel strategy under mild conditions (pH of 8.0 at room temperature). Using this strategy, DOTA-Mal was labeled by 68Ga before it reacted with the sulfhydryl group–containing biomolecules, which avoided damage to said biomolecules caused by the harsh reaction conditions required in 68Ga-labeling procedures. The biological and chemical properties of these three radiotracers synthesized using this strategy are well manifested. Through a series of experiments, the effectiveness of this strategy is demonstrated, and we believe that this site-specific bioactivity-friendly reaction strategy will facilitate developments and translation applications of varieties of 68Ga-labeled positron emission tomography probes.

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“…This may be due to the abnormal activity of fibroblasts in thrombosis and vascular occlusion. 5,6 In terms of cardiovascular disease, FAP is expressed in activated fibroblasts rather than quiescent fibroblasts. [7][8][9] This leads to a very low background signal in healthy tissue but intense activity in areas of activated fibroblasts with FAP expression.…”

mentioning

confidence: 99%

18F-FAPI-42 PET/CT Findings in a Patient With Left Ventricular Mural Thrombus

Wang,

Cheng,

Cui

et al. 2024

Clin Nucl Med

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18F-FAPI-42 PET/CT is a novel imaging tool targeting fibroblast activation protein (FAP). We describe the 18F-FAPI-42 PET/CT findings of a left ventricular mural thrombus in a 50-year-old man who had chest tightness. The 18F-FAPI-42 PET/CT showed annular uptake at the apex of the left ventricle, but there was no uptake of 18F-FDG. This case showed that abnormal 18F-FAPI-42 uptake in the heart may be associated with mural thrombus and should be evaluated clinically.

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Radiotracers to Address Unmet Clinical Needs in Cardiovascular Imaging, Part 2: Inflammation, Fibrosis, Thrombosis, Calcification, and Amyloidosis Imaging

Cited by 14 publications

References 85 publications

Regulatory Agencies and PET/CT Imaging in the Clinic

Regulatory Agencies and PET/CT Imaging in the Clinic

Exploration of ⁶⁸Ga-DOTA-MAL as a Versatile Vehicle for Facile Labeling of a Variety of Thiol-Containing Bioactive Molecules

18F-FAPI-42 PET/CT Findings in a Patient With Left Ventricular Mural Thrombus

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Radiotracers to Address Unmet Clinical Needs in Cardiovascular Imaging, Part 2: Inflammation, Fibrosis, Thrombosis, Calcification, and Amyloidosis Imaging

Cited by 14 publications

References 85 publications

Regulatory Agencies and PET/CT Imaging in the Clinic

Regulatory Agencies and PET/CT Imaging in the Clinic

Exploration of 68Ga-DOTA-MAL as a Versatile Vehicle for Facile Labeling of a Variety of Thiol-Containing Bioactive Molecules

18F-FAPI-42 PET/CT Findings in a Patient With Left Ventricular Mural Thrombus

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Exploration of ⁶⁸Ga-DOTA-MAL as a Versatile Vehicle for Facile Labeling of a Variety of Thiol-Containing Bioactive Molecules