Allen Barry J, Raja Chand, Rizvi Syed, Li Yong, Tsui Wendy, Graham Peter, Thompson John F, Reisfeld Ralph A, Kearsley John
Centre For Experimental Radiation Oncology, St. George Hospital, Kogarah, NSW 2217, Australia.
Cancer Biol Ther. 2005 Dec;4(12):1318-24. doi: 10.4161/cbt.4.12.2251. Epub 2005 Dec 18.
This paper reports the development and application of intralesional targeted alpha therapy (TAT) for melanoma, being the first part of a program to establish a new systemic therapy.
Labelling the benign targeting vector 9.2.27 with 213Bi forms the alpha-immunoconjugate (AIC), which is highly cytotoxic to targeted melanoma cells.
To investigate the safety and efficacy of intralesional AIC in patients with metastatic skin melanoma.
16 melanoma patients were recruited. All the patients were positive to the monoclonal antibody 9.2.27. AIC doses from 50 to 450 mCi injected into lesions of different sizes resulted in massive cell death, as observed by the presence of tumour debris. The AIC was very effective in delivering a high dose to the tumour while sparing other tissues. There were no significant changes in blood proteins and electrolytes. There was no evidence of a human-antimouse-antibody reaction. Evidence of significant decline in serum marker melanoma-inhibitory-activity protein (MIA) at 2 weeks post-TAT was observed.
Intralesional TAT for melanoma was found to be quite safe up to 450 mCi, and efficacious at a dose of 200 mCi. MIA, apoptosis and ki67 proliferation marker tests all indicated that TAT is a promising therapy for the control of inoperable secondary melanoma or primary ocular melanoma.
本文报道了瘤内靶向α治疗(TAT)在黑色素瘤中的研发与应用,这是建立一种新的全身治疗方案的项目的第一部分。
用²¹³Bi标记良性靶向载体9.2.27可形成α免疫偶联物(AIC),其对靶向的黑色素瘤细胞具有高度细胞毒性。
研究瘤内注射AIC治疗转移性皮肤黑色素瘤患者的安全性和有效性。
招募了16例黑色素瘤患者。所有患者对单克隆抗体9.2.27均呈阳性。向不同大小的病灶内注射50至450毫居里的AIC剂量导致大量细胞死亡,从肿瘤碎片的存在情况可观察到这一点。AIC在向肿瘤递送高剂量药物的同时能使其他组织免受影响,效果显著。血液蛋白质和电解质无明显变化。没有证据表明存在人抗鼠抗体反应。在TAT后2周观察到血清标志物黑色素瘤抑制活性蛋白(MIA)显著下降。
发现瘤内TAT治疗黑色素瘤在高达450毫居里的剂量下相当安全,200毫居里的剂量有效。MIA、凋亡和ki67增殖标志物检测均表明TAT是控制无法手术的继发性黑色素瘤或原发性眼黑色素瘤的一种有前景的治疗方法。