更新于：2024-11-21

[18F] fluorobisphenol-A

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

别名

靶点-

作用机制-

治疗领域-

在研适应症-

非在研适应症-

原研机构

Ground Fluor Pharmaceuticals, Inc.

在研机构-

非在研机构

Ground Fluor Pharmaceuticals, Inc.

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

项与 [18F] fluorobisphenol-A 相关的临床试验

JPRN-jRCTs031180302 / Completed临床2期IIT

Clinical study to evaluate the usefulness of 18F-FBPA-PET for patient selection and expanding indication for BNCT

开始日期2017-01-04

申办/合作机构-

JPRN-UMIN000035976 / RecruitingIIT

Clinical study to evaluate the usefulness of 18F-FBPA-PET for patient selection and expanding indication for BNCT - Usefulness of 18F-FBPA-PET

开始日期2017-01-04

申办/合作机构-

100 项与 [18F] fluorobisphenol-A 相关的临床结果

登录后查看更多信息

100 项与 [18F] fluorobisphenol-A 相关的转化医学

登录后查看更多信息

100 项与 [18F] fluorobisphenol-A 相关的专利（医药）

登录后查看更多信息

项与 [18F] fluorobisphenol-A 相关的文献（医药）

2019-04-01·Annals of Nuclear Medicine4区 · 医学

4-Borono-2-18F-fluoro-l-phenylalanine PET for boron neutron capture therapy-oriented diagnosis: overview of a quarter century of research

4区 · 医学

Review

作者: Ishiwata, Kiichi

4-¹⁰B-Borono-2-¹⁸F-fluoro-L-phenylalanine (¹⁸F-FBPA) was developed for monitoring the pharmacokinetics of 4-¹⁰B-borono-L-phenylalanine (¹⁰B-BPA) used in boron neutron capture therapy (BNCT) with positron emission tomography (PET). The tumor-imaging potential of ¹⁸F-FBPA was demonstrated in various animal models. Accumulation of ¹⁸F-FBPA was higher in melanomas than in non-melanoma tumors in animal models and cell cultures. ¹⁸F-FBPA was incorporated into tumors mediated mainly by L-type amino acid transporters in in vitro and in vivo models. Tumoral distribution of ¹⁸F-FBPA was primarily related to the activity of DNA synthesis. ¹⁸F-FBPA is metabolically stable but is incorporated into melanogenesis non-enzymatically. These in vitro and in vivo characteristics of ¹⁸F-FBPA corresponded well to those of ¹⁰B-BPA. Nuclear magnetic resonance and other studies using non-radioactive ¹⁹F-^10/11B-FBPA also contributed to characterization. The validity and reliability of ^18/19F-FBPA as an in vivo probe of ¹⁰B-BPA were confirmed by comparison of the pharmacokinetics of ¹⁸F-FBPA and ¹⁰B-BPA and direct measurement of both ¹⁸F and ¹⁰B in tumors with various doses of both probes administered by different routes and methods. Clinically, based on the kinetic parameters of dynamic ¹⁸F-FBPA PET, the estimated ¹⁰B-concentrations in tumors with continuous ¹⁰B-BPA infusion were similar to those measured directly in surgical specimens. The significance of ¹⁸F-FBPA PET was verified for the estimation of ¹⁰B-concentration and planning of BNCT. Later ¹⁸F-FBPA PET has been involved in ¹⁰B-BPA BNCT of patients with intractable tumors such as malignant brain tumors, head and neck tumors, and melanoma. Usually a static PET scan is used for screening patients for BNCT, prediction of the distribution and accumulation of ¹⁰B-BPA, and evaluation of treatment after BNCT. In some clinical trials, a tumor-to-normal tissue ratio of ¹⁸F-FBPA > 2.5 was an inclusion criterion for BNCT. Apart from BNCT, ¹⁸F-FBPA was demonstrated to be a useful PET probe for tumor diagnosis in nuclear medicine: better tumor-to-normal brain contrast compared with ¹¹C-methionine, differentiation of recurrent and radiation necrosis after radiotherapy, and melanoma-preferential uptake. Further progress in ¹⁸F-FBPA studies is expected for more elaborate evaluation of ¹⁰B-concentrations in tumors and normal tissues for successful ¹⁰B-BPA BNCT and for radiosynthesis of ¹⁸F-FBPA to enable higher ¹⁸F-activity amounts and higher molar activities.

2018-05-01·Cancer Science2区 · 医学

Non‐invasive estimation of ¹⁰B‐4‐borono‐L‐phenylalanine‐derived boron concentration in tumors by PET using 4‐borono‐2‐¹⁸F‐fluoro‐phenylalanine

2区 · 医学

ArticleOA

作者: Nakamura, Satoshi ; Itami, Jun ; Honda, Natsuki ; Shikano, Naoto ; Ito, Masashi ; Fujii, Hirofumi ; Kurihara, Hiroaki ; Hiroi, Kenta ; Yoshimoto, Mitsuyoshi

In boron neutron capture therapy (BNCT), 10B‐4‐borono‐L‐phenylalanine (BPA) is commonly used as a 10B carrier. PET using 4‐borono‐2‐18F‐fluoro‐phenylalanine (18F‐FBPA PET) has been performed to estimate boron concentration and predict the therapeutic effects of BNCT; however, the association between tumor uptake of 18F‐FBPA and boron concentration in tumors remains unclear. The present study investigated the transport mechanism of 18F‐FBPA and BPA, and evaluated the utility of 18F‐FBPA PET in predicting boron concentration in tumors. The transporter assay revealed that 2‐aminobicyclo‐(2.2.1)‐heptane‐2‐carboxylic acid, an inhibitor of the L‐type amino acid transporter, significantly inhibited 18F‐FBPA and 14C‐4‐borono‐L‐phenylalanine (14C‐BPA) uptake in FaDu and LN‐229 human cancer cells. 18F‐FBPA uptake strongly correlated with 14C‐BPA uptake in 7 human tumor cell lines (r = .93; P < .01). PET experiments demonstrated that tumor uptake of 18F‐FBPA was independent of the administration method, and uptake of 18F‐FBPA by bolus injection correlated well with BPA uptake by continuous intravenous infusion. The results of this study revealed that evaluating tumor uptake of 18F‐FBPA by PET was useful for estimating 10B concentration in tumors.

100 项与 [18F] fluorobisphenol-A 相关的药物交易

登录后查看更多信息