Joung J Y, Ha Y S, Kim I Y
Section of Urologic Oncology and the Dean and Betty Gallo Prostate Cancer Center, The Cancer Institute of New Jersey, Robert Wood Johnson Medical School, New Brunswick, New Jersey, USA; Department of Urology, Center for Prostate Cancer, National Cancer Center, Goyang, Korea.
Drugs Today (Barc). 2013 Aug;49(8):483-90. doi: 10.1358/dot.2013.49.8.1968670.
Radium Ra 223 dichloride (Xofigo®, formerly Alpharadin) is one of the representative α-particle-emitting isotopes that delivers radiation with a higher biological effect to a more localized area. Preclinical studies in mouse, rat and canine models have demonstrated that radium Ra 223 dichloride has a definite skeletal affinity and antitumor effect with a relatively low toxicity on bone marrow. More recently, in a large randomized phase III trial (ALSYMPCA), patients with bone metastasis and castration-resistant prostate cancer (CRPC) received six cycles of 50 kBq/kg of radium Ra 223 dichloride in 4-week intervals. In these men, radium Ra 223 dichloride improved the median overall survival by 3.6 months when compared to the placebo group. Collectively, these results suggest that radium Ra 223 dichloride is a promising candidate for managing bone metastases in patients with CRPC.
二氯化镭Ra 223(Xofigo®,原称Alpharadin)是一种典型的发射α粒子的同位素,它能在更局限的区域释放具有更高生物学效应的辐射。在小鼠、大鼠和犬模型上进行的临床前研究表明,二氯化镭Ra 223对骨骼具有明确的亲和性且有抗肿瘤作用,对骨髓的毒性相对较低。最近,在一项大型随机III期试验(ALSYMPCA)中,骨转移且去势抵抗性前列腺癌(CRPC)患者每4周接受6个周期、剂量为50 kBq/kg的二氯化镭Ra 223治疗。与安慰剂组相比,这些男性患者使用二氯化镭Ra 223后,中位总生存期延长了3.6个月。总体而言,这些结果表明,二氯化镭Ra 223有望用于治疗CRPC患者的骨转移。