DeNardo G L, Krohn K A, DeNardo S J
Cancer. 1977 Dec;40(6):2923-9. doi: 10.1002/1097-0142(197712)40:6<2923::aid-cncr2820400625>3.0.co;2-q.
The pharmacokinetics of 67Ga-citrate, 111In-bleomycin, *I-bleomycin, and *I-fibrinogen were compared in a murine KHJJ tumor model in order to assess their relative potential as agents for in vivo detection of cancer. Although all four agents have been reported to be clinically efficacious, in this tumor model, *I-fibrinogen and 67Ga-citrate had the greatest tumor accumulation with maximum concentrations of 11.7% and 10.5% respectively. However, both these radiopharmaceuticals cleared slowly from the blood and animal. The maximum tumor concentrations of 111In-bleomycin and *I-bleomycin were 2.9% and 2.6% respectively, but *I-bleomycin had the advantage of rapid clearance from the blood and animal. 67Ga-citrate did not achieve its maximum tumor concentration until 24 hours after administration, whereas the other radiopharmaceuticals achieved maximum tumor concentration within several hours of administration. From these observations 123I-bleomycin seems to deserve clinical trials in patients. 123I-fibrinogen appears to have significant oncophilic potential if its clearance from the animal can be accelerated without altering its accumulation in the tumor.
为了评估67Ga - 柠檬酸盐、111In - 博来霉素、123I - 博来霉素和123I - 纤维蛋白原作为体内癌症检测剂的相对潜力，在小鼠KHJJ肿瘤模型中比较了它们的药代动力学。虽然据报道所有这四种药剂在临床上都是有效的，但在这个肿瘤模型中，123I - 纤维蛋白原和67Ga - 柠檬酸盐在肿瘤中的积累最多，最大浓度分别为11.7%和10.5%。然而，这两种放射性药物从血液和动物体内清除缓慢。111In - 博来霉素和123I - 博来霉素在肿瘤中的最大浓度分别为2.9%和2.6%，但123I - 博来霉素具有从血液和动物体内快速清除的优势。67Ga - 柠檬酸盐直到给药后24小时才达到其在肿瘤中的最大浓度，而其他放射性药物在给药后几小时内就达到了最大肿瘤浓度。从这些观察结果来看，123I - 博来霉素似乎值得在患者中进行临床试验。如果123I - 纤维蛋白原能够在不改变其在肿瘤中积累的情况下加速从动物体内清除，那么它似乎具有显著的亲肿瘤潜力。
