Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India.
Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India.
Curr Med Chem. 2020;27(19):3187-3249. doi: 10.2174/0929867326666190201142814.
Bone pain arising from secondary skeletal malignancy constitutes one of the most common types of chronic pain among patients with cancer which can lead to rapid deterioration of the quality of life. Radionuclide therapy using bone-seeking radiopharmaceuticals based on the concept of localization of the agent at bone metastases sites to deliver focal cytotoxic levels of radiation emerged as an effective treatment modality for the palliation of symptomatic bone metastases. Bone-seeking radiopharmaceuticals not only provide palliative benefit but also improve clinical outcomes in terms of overall and progression-free survival. There is a steadily expanding list of therapeutic radionuclides which are used or can potentially be used in either ionic form or in combination with carrier molecules for the management of bone metastases. This article offers a narrative review of the armamentarium of bone-targeting radiopharmaceuticals based on currently approved investigational and potentially useful radionuclides and examines their efficacy for the treatment of painful skeletal metastases. In addition, the article also highlights the processes, opportunities, and challenges involved in the development of bone-seeking radiopharmaceuticals. Radium-223 is the first agent in this class to show an overall survival advantage in Castration-Resistant Prostate Cancer (CRPC) patients with bone metastases. This review summarizes recent advances, current clinical practice using radiopharmaceuticals for bone pain palliation, and the expected future prospects in this field.
骨转移继发恶性肿瘤引起的骨痛是癌症患者最常见的慢性疼痛类型之一，可导致生活质量迅速恶化。基于放射性药物在骨转移部位定位的概念，采用骨靶向放射性药物进行放射性核素治疗，已成为缓解骨转移症状的有效治疗方法。骨靶向放射性药物不仅提供姑息治疗益处，而且在总生存和无进展生存方面改善临床结局。有越来越多的治疗性放射性核素可用于或可能用于离子形式或与载体分子结合，以管理骨转移。本文对基于目前批准的研究性和潜在有用放射性核素的骨靶向放射性药物进行了叙述性综述，并检查了它们治疗骨转移疼痛的疗效。此外，本文还强调了骨靶向放射性药物开发所涉及的过程、机会和挑战。镭-223 是该类药物中第一个在去势抵抗性前列腺癌（CRPC）伴骨转移患者中显示出总生存优势的药物。本综述总结了该领域的最新进展、目前使用放射性药物缓解骨痛的临床实践以及预期的未来前景。
