Synthesis of 2′-fluoro-5-[11C]-methyl-1-β-d-arabinofuranosyluracil ([11C]-FMAU): A potential nucleoside analog for in vivo study of cellular proliferation with PET

Conti, Peter S.; Alauddin, Mian M.; Fissekis, John D.; Schmall, Bernard; Watanabe, K. A.

doi:10.1016/0969-8051(95)00017-r

Cited by 118 publications

(57 citation statements)

References 16 publications

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“…Cell culture studies showed it is incorporated into DNA (8). Later, it was labeled with 11 C to be used as a PET agent (9) and was tested in mice (10). A method for synthesis for 18 F-FMAU was developed (11)(12)(13), and this agent was studied in dogs, rats, and human subjects (14)(15)(16).…”

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confidence: 99%

Tumor Imaging Using 1-(2'-deoxy-2'-18F- Fluoro- -D-Arabinofuranosyl)Thymine and PET

Tehrani¹,

Muzik²,

Heilbrun³

et al. 2007

Journal of Nuclear Medicine

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The kinetics of 1-(29-deoxy-29-fluoro-b-D-arabinofuranosyl)thymine (FMAU) were studied using PET to determine the most appropriate and simplest approach to image acquisition and analysis. The concept of tumor retention ratio (TRR) is introduced and validated. Methods: Ten patients with brain (n 5 4) or prostate (n 5 6) tumors were imaged using 18 F-FMAU PET (mean dose, 369 MBq). Sixty-minute dynamic images were obtained; this was followed by whole-body images. Mean and maximum standardized uptake values (SUVmean and SUVmax, respectively) of each tumor were determined as the mean over 3 planes of each time interval. For kinetic analyses, blood activity was measured in 18 samples over 60 min. Samples were analyzed by high-performance liquid chromatography at 3 selected times to determine tracer metabolites. FMAU kinetics were measured using a 3-compartment model yielding the flux (K1 · k3/(k2 1 k3)) (K1, k2, and k3 are rate constants) and compared with TRR measurements. TRR was calculated as the tumor 18 F-FMAU uptake area under the curve divided by the product of blood 18 F-FMAU AUC and time. A similar analysis was performed using muscle to estimate 18 F-FMAU delivery. Results: SUVmean measurements obtained from 5 to 11 min correlated with those obtained from 30 to 60 min (r 2 5 0.92, P , 0.0001) and 50 to 60 min (r 2 5 0.92, P , 0.0001) due to the rapid clearance of 18 F-FMAU. Similar results were obtained using SUVmax measurements (r 2 5 0.93, P , 0.0001; r 2 5 0.88, P , 0.0001, respectively). The measurement of TRR using either blood or muscle activity over 11 min provided results comparable to those of 60-min dynamic imaging and a 3-compartment model. This analysis required only 5 blood samples drawn at 1, 2, 3, 5, and 11 min without metabolite correction to produce comparable results. Conclusion: Tissue retention ratio measurements obtained over 11 min can replace flux measurements in 18 F-FMAU imaging. The SUVmean and the SUVmax in 5-11 min images correlated well with those of images obtained at 50-60 min. The quality of the images and tissue kinetics in 11 min of imaging makes it a desirable and shorter tumor imaging option.

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confidence: 99%

Tumor Imaging Using 1-(2'-deoxy-2'-18F- Fluoro- -D-Arabinofuranosyl)Thymine and PET

Tehrani¹,

Muzik²,

Heilbrun³

et al. 2007

Journal of Nuclear Medicine

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“…The next task is to prepare starting material to send to Moravek Biochemicals, Inc for preparation of 1-N-[1 4 C]methyl-pseudouridine. The problem that arose in this task is after detailed assessment of the 14C-labeling issues, Moravek Biochemicals provided a final quotation that exceeded the budget established ($9000) for this task.…”

Section: Bodymentioning

confidence: 99%

“…This material must be first synthesized in unlabeled form, then as a 1 4 C-labeled compound. 1-N-[1 4 C]Methyl-pseudouridine will be tested in vitro. Depending on the in vitro results, then will undertake to prepare the " lC-labeled derivative for in vivo micro-PET (Positron Emission Tomography) imaging studies.…”

Section: Bodymentioning

confidence: 99%

New Positron-Emitting Probe for Imaging Cell Proliferation in Breast Cancer

Balatoni¹

2005

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“…11 However, C-11 labeled radiopharmaceuticals are of limited clinical application due to their short half-life (t1/2 = 20 min). 12 Therefore, the analogues labeled with longer half-life radioactive atom, such as fluorine-18 (t 1/2 = 110 min), are optimum for effective clinical application. Some of the fluorinated analogues of pyrimidine nucleosides have been studied as potential agents for imaging tumor cell proliferation or HSV1-TK reporter gene expression.…”

Section: Introductionmentioning

confidence: 99%

“…Some of the fluorinated analogues of pyrimidine nucleosides have been studied as potential agents for imaging tumor cell proliferation or HSV1-TK reporter gene expression. [12][13][14] (Fig. 1), and evaluated their PET imaging properties in HSV1-TK gene expressing tumor-bearing mice.…”

Section: Introductionmentioning

confidence: 99%