Scheinberg David A, McDevitt Michael R
Department of Molecular Pharmacology and Chemistry, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue,New York, NY 10065, USA.
Curr Radiopharm. 2011 Oct;4(4):306-20. doi: 10.2174/1874471011104040306.
Alpha particle-emitting isotopes are being investigated in radioimmunotherapeutic applications because of their unparalleled cytotoxicity when targeted to cancer and their relative lack of toxicity towards untargeted normal tissue. Actinium- 225 has been developed into potent targeting drug constructs and is in clinical use against acute myelogenous leukemia. The key properties of the alpha particles generated by 225Ac are the following: i) limited range in tissue of a few cell diameters; ii) high linear energy transfer leading to dense radiation damage along each alpha track; iii) a 10 day halflife; and iv) four net alpha particles emitted per decay. Targeting 225Ac-drug constructs have potential in the treatment of cancer.
发射α粒子的同位素因其在靶向癌症时具有无与伦比的细胞毒性以及对未靶向的正常组织相对缺乏毒性,正在放射免疫治疗应用中进行研究。锕-225已被开发成有效的靶向药物构建体,并正在用于治疗急性髓性白血病的临床应用中。由225Ac产生的α粒子的关键特性如下:i)在组织中的射程有限,约为几个细胞直径;ii)高线性能量传递,导致沿每条α粒子径迹产生密集的辐射损伤;iii)半衰期为10天;iv)每次衰变发射四个净α粒子。靶向225Ac的药物构建体在癌症治疗中具有潜力。