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用于前列腺癌的镥Lu 177维泊妥珠单抗四钠。

Lutetium Lu 177 vipivotide tetraxetan for prostate cancer.

作者信息

Liu Xing, Fang Gao-Chuan, Lu Hao, Shi Zhen-Duo, Chen Zhe-Sheng, Han Cong-Hui

机构信息

Department of Urology, Xuzhou Clinical College of Xuzhou Medical University, Jiangsu, China.

Department of Urology, Xuzhou Central Hospital, Jiangsu, China.

出版信息

Drugs Today (Barc). 2023 Jan;59(1):37-49. doi: 10.1358/dot.2023.59.1.3476574.

Abstract

On March 23, 2022, the U.S. Food and Drug Administration (FDA) approved Pluvicto (lutetium Lu 177 vipivotide tetraxetan), also known as 177Lu-PSMA-617, for the treatment of adult patients with metastatic castration-resistant prostate cancer (mCRPC) who have highly expressed prostate-specific membrane antigen (PSMA) and have at least one metastatic lesion. It is the first FDA-approved targeted radioligand therapy for eligible men with PSMA-positive mCRPC. Lutetium Lu 177 vipivotide tetraxetan is a radioligand that strongly binds to PSMA, making it ideal for treating cancers of the prostate by targeted radiation, resulting in DNA damage and cell death. PSMA is overexpressed in cancer cells while being lowly expressed in normal tissues, which makes it an ideal theranostic target. As precision medicine advances, this is a thrilling turning point for highly individualized treatments. This review aims to summarize the pharmacology and clinical studies of the novel drug lutetium Lu 177 vipivotide tetraxetan for the treatment of mCRPC, emphasizing its mechanism of action, pharmacokinetics and safety.

摘要

2022年3月23日,美国食品药品监督管理局(FDA)批准了Pluvicto(镥Lu 177 维泊妥珠单抗四钠),也称为177Lu-PSMA-617,用于治疗患有转移性去势抵抗性前列腺癌(mCRPC)且前列腺特异性膜抗原(PSMA)高表达且至少有一处转移病灶的成年患者。它是FDA批准的首个用于符合条件的PSMA阳性mCRPC男性患者的靶向放射性配体疗法。镥Lu 177维泊妥珠单抗四钠是一种放射性配体,它能与PSMA紧密结合,使其成为通过靶向放射治疗前列腺癌的理想药物,从而导致DNA损伤和细胞死亡。PSMA在癌细胞中过度表达,而在正常组织中低表达,这使其成为理想的治疗诊断靶点。随着精准医学的发展,这对于高度个体化治疗来说是一个激动人心的转折点。本综述旨在总结新型药物镥Lu 177维泊妥珠单抗四钠治疗mCRPC的药理学和临床研究,重点阐述其作用机制、药代动力学和安全性。

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