Fluorine-18-fluorocyclopropylhexadecanoic acid(Fluorine-18-fluorocyclopropylhexadecanoic acid)

概要

基本信息

药物类型

小分子化药、诊断用放射药物

别名

18F-fluorocyclopropylhexadecanoic acid、CardioPET、FCPHA

+ [4]

靶点-

作用机制

PET imaging(正电子发射断层成像术增强剂)

治疗领域

心血管疾病

在研适应症

冠心病

非在研适应症-

原研机构

Mass General Brigham, Inc.

在研机构

Mass General Brigham, Inc.

Harvard Medical School

非在研机构

FluoroPharma, Inc.

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C18H33FO2

InChIKeyDDTRZLZETKPBPQ-CKNKWQFVSA-N

CAS号855927-17-2

关联

2

项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的临床试验

NCT01826773 / Completed临床2期

A Phase II Open-Labeled Study to Evaluate CardioPET™ as a PET Imaging Agent for Evaluation of Myocardial Perfusion and Fatty Acid Uptake in Subjects With Coronary Artery Disease

The study is designed to evaluate how safe and how well an investigational imaging product CardioPET™ performs as compared to standard approved imaging products in assessing the function of heart muscle in coronary artery disease patients.

开始日期2013-03-01

申办/合作机构

FluoroPharma, Inc.

NCT00413647 / Completed临床1期

A Phase I Study to Evaluate the Safety, Biodistribution and Radiation Dosimetry of CardioPET™ as a PET Tracer for Detection of Coronary Artery Disease

Safety and dosimetry of CardioPET™ will be evaluated in normal healthy volunteers and CAD subjects both male and female between the ages of 50-85. Nine normal controls will undergo repeated whole body imaging for biodistribution and dosimetry estimation. Six other normal healthy subjects will undergo heart imaging only. Six CAD subjects will undergo heart imaging only.

开始日期2006-09-01

申办/合作机构

FluoroPharma, Inc.

100 项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的临床结果

登录后查看更多信息

100 项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的转化医学

登录后查看更多信息

100 项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的专利（医药）

登录后查看更多信息

4

项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的文献（医药）

2015-01-01·Journal of Veterinary Diagnostic Investigation4区 · 农林科学

Analytical validation of a second-generation immunoassay for the quantification of N-terminal pro–B-type natriuretic peptide in canine blood

4区 · 农林科学

Article

作者: Cahill, Roberta J. ; Clark, Genevieve H. ; Drexel, Jan P. ; Pigeon, Kathleen ; Buch, Jesse S. ; Strong-Townsend, Marilyn I.

N-terminal pro–B-type natriuretic peptide (NT-proBNP) has been shown to have clinical utility as a biomarker in dogs with heart disease. There were several limitations associated with early diagnostic assay formats including a limited dynamic range and the need for protease inhibitors to maintain sample stability. A second-generation Cardiopet® proBNP enzyme-linked immunosorbent assay (IDEXX Laboratories Inc., Westbrook, Maine) was developed to address these limitations, and the present study reports the results of the analytical method validation for the second-generation assay. Coefficients of variation for intra-assay, interassay, and total precision based on 8 samples ranged from 3.9% to 8.9%, 2.0% to 5.0%, and 5.5% to 10.6%, respectively. Analytical sensitivity was established at 102 pmol/l. Accuracy averaged 102.0% based on the serial dilutions of 5 high-dose canine samples. Bilirubin, lipids, and hemoglobin had no effect on results. Reproducibility across 3 unique assay lots was excellent with an average coefficient of determination ( r2) of 0.99 and slope of 1.03. Both ethylenediamine tetra-acetic acid plasma and serum gave equivalent results at time of blood draw (slope = 1.02, r2 = 0.89; n = 51) but NT-proBNP was more stable in plasma at 25°C with median half-life measured at 244 hr and 136 hr for plasma and serum, respectively. Plasma is the preferred sample type and is considered stable up to 48 hr at room temperature whereas serum should be frozen or refrigerated when submitted for testing. Results of this study validate the second-generation canine Cardiopet proBNP assay for accurate and precise measurement of NT-proBNP in routine sample types from canine patients.

2005-02-01·Journal of nuclear medicine : official publication, Society of Nuclear Medicine

Evaluation of trans-9-18F-fluoro-3,4-Methyleneheptadecanoic acid as a PET tracer for myocardial fatty acid imaging.

Article

作者: Fischman, Alan J ; Elmaleh, David R ; Bonab, Ali A ; Shoup, Timothy M

This study describes the radiosynthesis and preliminary biologic evaluation of trans-9(RS)-(18)F-fluoro-3,4(RS,RS)-methyleneheptadecanoic acid ((18)F-FCPHA) as a new potential probe for assessing myocardial fatty acid metabolism by PET. This fatty acid, containing a cyclopropyl moiety in the beta,gamma-position, was designed to enter the myocardium by the same mechanism as natural fatty acids and to undergo partial metabolism before being trapped in the cell.METHODS(18)F-FCPHA and the beta-methyl analog 8(RS)-(18)F-fluoro-3(RS)-methylheptadecanoic acid ((18)F-FBMHA) were prepared from their corresponding mesylate precursors by nucleophilic substitution. The precursors used for labeling were fully characterized, and the data were consistent with the proposed structures. Biodistribution studies of each tracer were performed with Sprague-Dawley rats at 5 and 60 min after injection. Sequential imaging of a rhesus monkey injected with 222 MBq of (18)F-FCPHA was performed by use of a microPET camera.RESULTSAt 5 and 60 min, heart uptake values measured as mean +/- SD percentage injected dose per gram (%ID/g) in rats for (18)F-FCPHA were 1.55 +/- 0.72 and 1.43 +/- 0.14, respectively. The heart-to-blood ratios at 5 and 60 min, an indication of target definition, were 25.8 and 20.4, respectively. The heart-to-lung ratios at 5 and 60 min were 3.3 and 4.6, respectively. Bone accumulation (%ID/g), an indication of defluorination, was 0.16 +/- 0.03 at 5 min and increased to 0.70 +/- 0.39 at 60 min. The heart-to-blood ratio obtained with (18)F-FBMHA was 2.6 at 5 min and did not change significantly at 60 min. Imaging of the monkey heart after injection of (18)F-FCPHA showed an initial spike of activity corresponding to blood flow followed by a plateau at 10 min.CONCLUSIONThe cyclopropyl moiety in (18)F-FCPHA does have a significant influence on heart accumulation, as suggested by the high heart-to-blood ratio and the fast blood clearance in rats. These results, along with the remarkable quality of the PET images, indicate the potential of this new class of labeled fatty acids for use in studying heart disease by PET.

1996-02-01·Journal of nuclear medicine : official publication, Society of Nuclear Medicine

Feasibility of fluorine-18-fluorophenylalanine for tumor imaging compared with carbon-11-L-methionine.

Article

作者: Yamada, S ; Abe, Y ; Takahashi, J ; Ishiwata, K ; Fukuda, H ; Kubota, K ; Ido, T ; Kubota, R

L-[methyl-11C]methionine (11C-Met) is a useful tracer for tumor imaging with PET. The drawbacks include a short half-life and high physiological accumulation in abdominal organs. To overcome these shortfalls, the feasible use of [18F]fluorophenylalanine (18F-Phe), which shares the same amino acid transport system with Met, for tumor imaging was examined.METHODSThe time course of tissue distribution of 18F-Phe and the tumor uptake response to radiotherapy were compared with 14C-Met and [3H] thymidine (3H-Thd) in the rat AH109A tumor model. Intratumoral distribution of 18F-Phe was compared with 14C-Met and 14C-Thd using double-tracer macroautoradiography (ARG). We also evaluated whole-body ARG.RESULTSTumor uptake of 18F-Phe peaked at 60 min postinjection and was higher than that of the liver, intestine and kidney but lower than the pancreas. Tumor uptake of 18F-Phe was similar to that of 14C-Met. Tumor-to-blood and tumor-to-muscle ratios were higher in 14C-Met compared with that of 18F-Phe because of the rapid blood clearance of 14C-Met. With whole-body ARG, the tumor was clearly visualized with high contrast. Radiotherapeutic response of tumor uptake of 18F-Phe was as rapid as that with 14C-Met and with 3H-Thd. Intratumoral distribution of 18F-Phe and 14C-Met were identical, and 18F-Phe and 14C-Thd were similar.CONCLUSIONFluorine-18-Phe seems to be a potentially useful amino acid tracer for tumor imaging with a longer half-life than 11C, with higher tumor contrast in the abdomen than Met and a similar sensitive response to radiotherapy.

100 项与 Fluorine-18-fluorocyclopropylhexadecanoic acid 相关的药物交易

登录后查看更多信息