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更新于：2025-03-20

18F-RP-170

更新于：2025-03-20

概要

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-

作用方式-

作用机制-

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/序列

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）

2019-01-01·Cerebrovascular Diseases3区 · 医学

Reduced Hypoxic Tissue and Cognitive Improvement after Revascularization Surgery for Chronic Cerebral Ischemia

3区 · 医学

Article

作者: Fujiwara, Shunrou ; Kubo, Yoshitaka ; Ogasawara, Kuniaki ; Yoshida, Kenji ; Terasaki, Kazunori ; Shimada, Yasuyoshi ; Kobayashi, Masakazu ; Beppu, Takaaki

Background: Hypoxic but viable neural tissue is seen on 1-(2–18F-fluoro-1-[hydroxymethyl]ethoxy) methyl-2-nitroimidazole (18F-FRP170) positron emission tomography (PET) in patients with chronic cerebral ischemia with a combination of misery perfusion and moderately reduced oxygen metabolism. Cognitive function sometimes improves after revascularization surgery in patients with chronic cerebral ischemia. Objectives: We used brain perfusion single-photon emission computed tomography (SPECT) and 18F-FRP170 PET to determine whether hypoxic tissue was reduced following the restoration of cerebral perfusion after carotid endarterectomy (CEA) in patients with severe stenosis of the cervical internal carotid artery (ICA) and whether the reduction in hypoxic tissue was associated with cognitive improvement. Method: Eighteen patients with abnormally reduced cerebral blood flow (CBF) in the affected cerebral hemispheres on preoperative brain perfusion SPECT underwent CEA. They underwent 18F-FRP170 PET and neuropsychological tests preoperatively and 6 months postoperatively. Brain perfusion SPECT was also performed 6 months postoperatively. Regions of interest were placed in the bilateral middle cerebral artery territories on SPECT and PET images, and the ratio of values in the affected versus contralateral hemispheres was calculated. Results: The CBF ratio (p = 0.0006) and 18F-FRP170 ratio (p = 0.0084) were significantly increased and reduced, respectively, after surgery compared to the corresponding ratios before surgery. The difference in the 18F-FRP170 ratio (postoperative – preoperative value) was negatively correlated with the difference in the CBF ratio (ρ = –0.695; p = 0.0009). The difference in the 18F-FRP170 ratio was significantly lower in patients with postoperative improved cognition compared to that in those without (p = 0.0007). The area under the receiver operating characteristics curve for the difference in the 18F-FRP170 ratio for detecting postoperative improved cognition was significantly greater than that for the difference in the CBF ratio (difference between areas, 0.278; p = 0.0248). Conclusions: Hypoxic tissue is reduced following the restoration of cerebral perfusion with revascularization surgery in patients with severe atherosclerotic stenosis of the cervical ICA. The reduction in hypoxic tissue is associated with cognitive improvement in such patients.

2015-05-01·Annals of Nuclear Medicine4区 · 医学

High-uptake areas on positron emission tomography with the hypoxic radiotracer 18F-FRP170 in glioblastomas include regions retaining proliferative activity under hypoxia

4区 · 医学

Article

作者: Ogasawara, Kuniaki ; Takai, Yoshihiro ; Saura, Hiroaki ; Ehara, Shigeru ; Sasaki, Makoto ; Iwata, Ren ; Mtsuura, Hideki ; Beppu, Takaaki ; Sasaki, Toshiaki ; Terasaki, Kazunori

AbstractObjectiveThe aim was to evaluate the proliferative activity of high-uptake areas on positron emission tomography (PET) with the hypoxic cell radiotracer, 1-(2-[18F]fluoro-1-[hydroxymethyl]ethoxy)methyl-2-nitroimidazole (FRP170).MethodsThirteen patients with glioblastoma underwent FRP170 PET before tumor resection. During surgery, tumor specimens were stereotaxically obtained from regions corresponding to high (high-uptake areas, HUAs) and relatively low (low-uptake areas, LUAs) accumulation of FRP170. We compared immunohistochemical staining for Ki-67 and hypoxia-inducible factor (HIF)-1α between HUA and LUA.ResultsHIF-1α index was significantly higher in HUAs than in LUAs. In contrast, mean Ki-67 indices did not differ significantly between HUAs and LUAs.ConclusionsFindings for HIF-1α index clearly indicated that HUAs on FRP170 PET represented hypoxic regions in glioblastoma. However, findings of Ki-67 index suggest that HUAs on FRP170 PET include regions retaining proliferative activity regardless of tissue hypoxia.

2015-05-01·Stroke1区 · 医学

Hypoxic Viable Tissue in Human Chronic Cerebral Ischemia Because of Unilateral Major Cerebral Artery Steno-Occlusive Disease

1区 · 医学

Article

作者: Takai, Yoshihiro ; Beppu, Takaaki ; Saura, Hiroaki ; Yoshida, Koji ; Kobayashi, Masakazu ; Ogawa, Akira ; Yoshida, Kenji ; Terasaki, Kazunori ; Ogasawara, Kuniaki

Background and Purpose— Positron emission tomography (PET) with radiolabeled 2-nitroimidazoles directly detects hypoxic but viable tissue present in an acute ischemic area in the human brain. This study using PET with 1-(2- 18 F-fluoro-1-[hydroxymethyl]ethoxy) methyl-2-nitroimidazole ( 18 F-FRP170) aimed to determine whether tissue with an abnormally elevated uptake of 18 F-FRP170 exists in human chronic cerebral ischemia because of unilateral atherosclerotic major cerebral artery steno-occlusive disease. Methods—18 F-FRP170 PET was performed, and cerebral blood flow and metabolism were assessed using 15 O-gas PET in 20 healthy subjects and 52 patients. A region of interest (ROI) was automatically placed in 3 segments of the middle cerebral artery territory in both cerebral hemispheres with a 3-dimensional stereotaxic ROI template using SPM2, and each PET value was determined in each ROI. The ratio of values in the affected versus contralateral hemispheres was calculated for the 18 F-FRP170 PET image. Results— A significant correlation was observed between oxygen extraction fraction and 18 F-FRP170 ratios ( ρ =0.509; P <0.0001) in a total of 156 ROIs in 52 patients. The specificity and positive-predictive value for a combination of an elevated oxygen extraction fraction and a moderately reduced cerebral oxygen metabolism for detection of an abnormally elevated 18 F-FRP170 ratio (19 ROIs: 12%) were significantly greater than those for the individual categories (elevated oxygen extraction fraction, moderately reduced cerebral oxygen metabolism, or reduced cerebral blood flow). Conclusions— Tissues with abnormally elevated uptake of 18 F-FRP170 exist in human chronic cerebral ischemia characterized by a combination of misery perfusion and moderately reduced oxygen metabolism because of unilateral atherosclerotic major cerebral artery steno-occlusive disease.

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


ASTRO2005	N/A	缺氧	-	[18F]FRP-170 (WHT/Ht albino mice)	鏇簾構獵鑰觸衊夢構鬱(醖鹽選鹽選網構夢鏇艱) = very low, they are about 0.2 for thigh, heart, mediastinum and neck; higher (ca. 0.6) for liver and kidney 觸獵獵餘網艱蓋膚範廠 (製夢廠膚壓醖艱鹹醖憲 ) 更多	-	2005-10-01
				[18F]FRP-170 (Patients with recurrent esophageal cancer)