更新于：2024-11-21

18F-RP-170

更新于：2024-11-21

概要

研发状态

概要

基本信息

药物类型

小分子化药、诊断用放射药物

别名

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-

非在研适应症

心肌缺血

原研机构

Pola Chemical Industries, Inc.

在研机构-

非在研机构

Pola Chemical Industries, Inc.

最高研发阶段终止临床阶段不明

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C7H10FN3O4

InChIKeyAPIKHHGQEBCQED-COJKEBBMSA-N

CAS号291764-48-2

关联

项与 18F-RP-170 相关的临床试验

JPRN-jRCTs031190133 / Completed临床2期IIT

Clinical research on the superiority of 18F-FRP170 over 18F-FMISO for tumor hypoxia imaging

开始日期2019-11-13

申办/合作机构-

100 项与 18F-RP-170 相关的临床结果

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100 项与 18F-RP-170 相关的转化医学

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100 项与 18F-RP-170 相关的专利（医药）

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项与 18F-RP-170 相关的文献（医药）

2010-08-01·Journal of Neurosurgery1区 · 医学

Clinical article

1区 · 医学

Article

作者: Watanabe, Mika ; Takai, Yoshihiro ; Tominaga, Teiji ; Saito, Ryuta ; Takanami, Kentaro ; Kumabe, Toshihiro ; Higano, Shuichi ; Sonoda, Yukihiko ; Kanamori, Masayuki ; Shibahara, Ichiyo ; Iwata, Ren

ObjectAssessment of hypoxic conditions in brain tumors is important for predicting tumor aggressiveness and treatment response. A new hypoxia imaging agent, 1-(2-[18F]fluoro-1-[hydroxymethyl]ethoxy)methyl-2-nitroimidazole (FRP-170), with higher image contrast and faster clearance than preexisting hypoxia tracers for PET, was used to visualize hypoxic tissues in 8 patients with glioma.MethodsThe FRP-170 was injected and PET imaging was performed 2 hours later in 8 patients, including 3 with glioblastoma multiforme, 2 with oligodendroglioma, and 1 each with diffuse astrocytoma, anaplastic ganglioglioma, and recurrent anaplastic astrocytoma. All 8 patients also underwent MR imaging, and some patients underwent [11C]methionine or [18F]fluorodeoxyglucose PET, and proton MR spectroscopy for comparison. Tissues obtained at biopsy or radical resection were immunostained with hypoxia-inducible factor–1α (HIF-1α) antibody for the confirmation of hypoxia, except in the patient with recurrent anaplastic astrocytoma who was treated using Gamma Knife surgery.ResultsThe FRP-170 PET images showed marked uptake with upregulation of HIF-1α in the 3 glioblastomas multiforme, and moderate uptake in the recurrent anaplastic astrocytoma and one oligodendroglioma, but no uptake in the other tumors. The FRP-170 PET images showed positive correlation with HIF-1α immunoreactivity and some correlation with FDG PET and MR imaging enhancement, but no correlation with [11C]methionine PET. Imaging with FRP-170 PET seemed to be more sensitive for detecting hypoxia than identifying the lactate peak on proton MR spectroscopy.ConclusionsImaging with FRP-170 PET can visualize hypoxic lesions in patients with glioma, as confirmed by histological examination. This new method can assess tumor hypoxia preoperatively and noninvasively.

2005-02-01·Kaku igaku. The Japanese journal of nuclear medicine

[Development of [18F]FRP-170 injection for imaging hypoxia by PET].

Article

作者: Kudo, Yukitsuka ; Yamada, Shogo ; Furumoto, Shozo ; Funaki, Yoshihito ; Nakata, Eiko ; Ishikawa, Yoichi ; Hakamatsuka, Takashi ; Kaneta, Tomohiro ; Takai, Yoshihiro ; Iwata, Ren

A novel [18F]FRP-170 injection for imaging hypoxia by PET was developed for clinical use. The preparation was based on the simple on-column basic-hydrolysis and the whole procedure was automated by detecting He flow change for transferring and evaporating liquids. [18F]FRP-170 was prepared in around 15-20% decay-corrected radiochemical yield within 60 min and stable in saline for more than 6 hr. Radiochemical purity was over 99% and specific activity at EOS was 40-60 GBq/micromol. The radiation-absorbed dose to the whole body was estimated to be 1.0 mSv/185 MBq. The [18F]FRP-170 injection proved to be suitable for clinical use without acute toxicity or mutagenicity.

2002-01-01·Journal of nuclear medicine : official publication, Society of Nuclear Medicine

Imaging of ischemic but viable myocardium using a new 18F-labeled 2-nitroimidazole analog, 18F-FRP170.

Article

作者: Takahashi, Shoki ; Kagaya, Yutaka ; Yamada, Shogo ; Yamane, Yuriko ; Yuki, Masahiro ; Wada, Hiroaki ; Iwata, Ren ; Tsujitani, Michihiko ; Kaneta, Tomohiro ; Takai, Yoshihiro

RP170, 1-(2-hydroxy-1-[hydroxymethyl]ethoxy)methyl-2-nitroimidazole, is a new hypoxic radiosensitizer. We recently succeeded in labeling this compound with 18F to make 18F-FRP170, 1-(2-fluoro-1-[hydroxymethyl]ethoxy)methyl-2-nitroimidazole. In this study, we attempted to visualize the ischemic but viable myocardium of rats as hot-spot images using 18F-FRP170. We also compared the distribution of 18F-FRP170 with myocardial perfusion, fatty acid metabolism, and glucose metabolism.METHODSIn open-chest rats, the left coronary artery was ligated to make an ischemic myocardial model. We evaluated the myocardial accumulation of radiotracers by the double-tracer autoradiography technique. 14C-Iodoantipyrine (IAP), 125I-15-(p-iodophenyl)-3-(R,S)-methylpentadecanoic acid (BMIPP), and 14C-deoxyglucose (DG) were used as markers of myocardial perfusion, fatty acid metabolism, and glucose metabolism, respectively. Approximately 80 small circular regions of interest were placed throughout the left ventricular wall of the midventricular level section. The uptake in each region of interest was expressed as the percentage uptake of the average count in the remote area. We then defined the 18F-FRP170 high-uptake area (H-FRP) as that area where the percentage of FRP was >120% and the 18F-FRP170 low-uptake area (L-FRP) as that area where the percentage of FRP was <80%.RESULTSOn the 18F-FRP170 image of the ischemic myocardium, there was a low-uptake area in the center, which was bounded by a high-uptake area. The percentages of IAP in the H-FRP and the L-FRP were 48.5% +/- 5.8% and 2.2% +/- 0.2%, respectively; the percentages of BMIPP in the H-FRP and the L-FRP were 46.8% +/- 3.1% and 4.3% +/- 0.4%, respectively; and the percentages of DG in the H-FRP and the L-FRP were 107.0% +/- 6.8% and 4.3% +/- 0.4%, respectively. In diabetic rats, the percentages of DG in the H-FRP and the L-FRP were 407.7% +/- 14.9% and 72.5% +/- 5.0%, respectively, but the remote area on the DG image was insufficiently visualized. Histologic data using 2,3,5-triphenyltetrazolium chloride staining suggest that the high-uptake areas on 18F-FRP170 images reflect ischemic but viable myocardium.CONCLUSIONWe succeeded in visualizing the ischemic but viable myocardium as a hot spot on the 18F-FRP170 image. 18F-FRP170 can be expected to provide important information for determining the necessity of coronary intervention in ischemic heart disease patients, including diabetic patients.

100 项与 18F-RP-170 相关的药物交易

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研发状态

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASTRO	N/A	缺氧	-	[18F]FRP-170 (WHT/Ht albino mice)	鹹糧範淵遞夢夢蓋簾願(鹹廠顧網網壓繭觸衊憲) = very low, they are about 0.2 for thigh, heart, mediastinum and neck; higher (ca. 0.6) for liver and kidney 糧範築窪襯鹹夢艱積齋 (鏇鹽窪衊繭憲製鑰網糧 ) 更多	-	2005-10-01
				[18F]FRP-170 (Patients with recurrent esophageal cancer)