PET/Computed Tomography Using New Radiopharmaceuticals in Targeted Therapy

Sharma, Punit; Kumar, Rakesh; Alavi, Abass

doi:10.1016/j.cpet.2015.05.007

Cited by 7 publications

(2 citation statements)

References 78 publications

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“…Among the radiotracers used for PET imaging, 18 F-fluorodeoxyglucose (FDG) has played a remarkable role in staging, restaging, detecting recurrences, and predicting the prognosis of various cancers [ 1 ]. Although 18 F-FDG is still a key radiotracer, recently, radiopharmaceuticals other than 18 F-FDG have been thoroughly investigated to predict and monitor therapeutic responses along with the development of targeted therapies [ 2 ]. Radioisotopes with short half-lives, such as 18 F (t 1/2 = 110 min), 11 C (t 1/2 = 20 min) and 13 N (t 1/2 = 10 min), which are common in clinical practice, have the advantage of low radiation exposure.…”

Section: Introductionmentioning

confidence: 99%

Current Perspectives on 89Zr-PET Imaging

Yoon

Park

Ryu

et al. 2020

IJMS

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89Zr is an emerging radionuclide that plays an essential role in immuno-positron emission tomography (PET) imaging. The long half-life of 89Zr (t1/2 = 3.3 days) is favorable for evaluating the in vivo distribution of monoclonal antibodies. Thus, the use of 89Zr is promising for monitoring antibody-based cancer therapies. Immuno-PET combines the sensitivity of PET with the specificity of antibodies. A number of studies have been conducted to investigate the feasibility of 89Zr immuno-PET imaging for predicting the efficacy of radioimmunotherapy and antibody therapies, imaging target expression, detecting target-expressing tumors, and the monitoring of anti-cancer chemotherapies. In this review, we summarize the current status of PET imaging using 89Zr in both preclinical and clinical studies by highlighting the use of immuno-PET for the targets of high clinical relevance. We also present 89Zr-PET applications other than immuno-PET, such as nanoparticle imaging and cell tracking. Finally, we discuss the limitations and the ongoing research being performed to overcome the remaining hurdles.

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Section: Introductionmentioning

confidence: 99%

Current Perspectives on 89Zr-PET Imaging

Yoon

Park

Ryu

et al. 2020

IJMS

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“…Several PET radiotracers have been developed with the purpose of evaluating the functional or molecular changes associated with tumour biology [ 9 , 10 ]. To achieve this, it is necessary to find a specific target on tumour cells, as well as a radiotracer with high affinity and specificity for this target [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

Automated One-pot Radiosynthesis of [11C]S-adenosyl Methionine

Zoppolo

Porcal

Oliver

et al. 2017

CRP

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Background: Glycine N-methyltransferase is an enzyme overexpressed in some neo-plastic tissues. It catalyses the methylation of glycine using S-adenosyl methionine (SAM or AdoM-et) as substrate. SAM is involved in a great variety of biochemical processes, including transmeth-ylation reactions. Thus, [11C]SAM could be used to evaluate transmethylation activity in tumours. The only method reported for [11C]SAM synthesis is an enzymatic process with several limitations. We propose a new chemical method to obtain [11C]SAM, through a one-pot synthesis.Method: The optimization of [11C]SAM synthesis was carried out in the automated TRACERlab® FX C Pro module. Different labelling conditions were performed varying methylating agent, precur-sor amount, temperature and reaction time. The compound was purified using a semi-preparative HPLC. Radiochemical stability, lipophilicity and plasma protein binding were evaluated.Results: The optimum labelling conditions were [11C]CH3OTf as the methylating agent, 5 mg of precursor dissolved in formic acid at 60 ºC for 1 minute. [11C]SAM was obtained as a diastereomer-ic mixture. Three batches were produced and quality control was performed according to specifica-tions. [11C]SAM was stable in final formulation and in plasma. Log POCT obtained for [11C]SAM was (-2,01 ± 0,07) (n=4), and its value for plasma protein binding was low.Conclusion: A new chemical method to produce [11C]SAM was optimized. The radiotracer was ob-tained as a diastereomeric mixture with a 53:47 [(R,S)-isomer: (S,S)-isomer] ratio. The compound was within the quality control specifications. In vitro stability was verified. This compound is suita-ble to perform preclinical and clinical evaluations.

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