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Rhenium-188 based radiopharmaceuticals for treatment of liver tumours

机译:基于Rhenium-188的放射性药物治疗肝肿瘤

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摘要

Rhenium-188 (~188Re) is a high energy beta-emitter with a physical half life of 17 hours. Various ~188Re based radiopharmaceuticals were developed to treat liver malignancies. The vast majority of studies focus on patients suffering from hepatocellular carcinoma (HCC). Most radiopharmaceuticals are based on Lipiodol as a vehicle for the rhenium-188. The radiopharmaceutical that was tested clinically in detail is the ~~188Re-HDD/Lipiodol, developed by the Seoul University. Clinical data derived from several phase I and II studies using ~188Re-HDD/Lipiodol suggest an excellent tolerance in patients with Child-Pugh A cirrhosis. A shortcoming in some trials was the occasional low labelling efficiency of ~188Re-HDD/Lipiodol. Some newer ~188Re based radiopharmaceuticals claim to have consistent high labelling efficiencies, however clinical data for these compounds are scarce or lacking at this moment. Hopefully, phase I clinical data will become available for promising radiopharmaceuticals such as ~188Re-SSS-Lipiodol, developed by the group of Rennes, in the upcoming years. In Dresden a very different approach is used. They labelled human serum albumin microspheres with high activities of ~188Re. In a small group of patients with liver metastasis and a few HCC patients, treatment proved safe. In the present clinical field, ~188Re-based radiopharmaceuticals will have to proof firmly their strength and reliability in large patient groups if they want to compete with the commercially available yttrium-90 microspheres.
机译:hen 188(〜188Re)是高能β发射极,物理半衰期为17小时。已开发出各种基于〜188Re的放射性药物来治疗肝恶性肿瘤。绝大多数研究集中于患有肝细胞癌(HCC)的患者。大多数放射性药物都基于Lipiodol作为as 188的载体。由首尔大学开发的〜188Re-HDD / Lipiodol是经过临床详细测试的放射性药物。来自一些使用〜188Re-HDD / Lipiodol进行的I和II期研究的临床数据表明,Child-Pugh A肝硬化患者具有极好的耐受性。一些试验的缺点是偶尔出现〜188Re-HDD / Lipiodol的低标记效率。一些较新的基于〜188Re的放射性药物声称具有一致的高标记效率,但是目前这些化合物的临床数据稀少或缺乏。希望在未来几年中,有前途的放射性药物(如〜188Re-SSS-Lipiodol)将获得雷诺集团开发的I期临床数据。在德累斯顿,使用了一种非常不同的方法。他们用〜188Re的高活性标记了人血清白蛋白微球。在少数肝转移患者和少数HCC患者中,治疗被证明是安全的。在当前的临床领域中,如果要与商业上可买到的yttrium-90微球竞争,基于〜188Re的放射性药物必须在大型患者组中牢固地证明其强度和可靠性。

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