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标有Lu-177-标记的异构对等剂,针对PSMA和骨转移,用于放射性核素治疗

Zhihao Zha¹, Karl Ploessl¹, Seok Rye Choi¹

¹Five Eleven Pharma Inc., Philadelphia, Pennsylvania 19104, United States.

Journal of medicinal chemistry

|September 5, 2023

概括

针对前列腺特异性膜抗原 (PSMA) 和骨转移的新型异质双价药物显示出前列腺癌治疗的前景. [177Lu]Lu-P17-079证明了双重准能力,可以改进治疗策略.

科学领域:

核医学是一种核医学.
在瘤学瘤学.
放射性药物化学放射性药物化学

背景情况:

前列腺特异性膜抗原 (PSMA) 是前列腺癌成像和治疗的验证标.
最近FDA对[177Lu]Lu-PSMA-617 (Pluvicto) 的批准强调了PSMA向放射性核酸治疗的临床潜力.
前列腺癌往往转移到骨,需要治疗策略,以解决原发性瘤和骨损伤.

研究的目的:

开发能够同时针对PSMA和骨转移的新型异质双价放射性药剂.
评估这些新药物在临床前前列腺癌模型中的体内生物分布和向能力.

主要方法:

合成和表征两种新型异质双价剂,标记为卢-177 ([177Lu]Lu-P17-079和[177Lu]Lu-P17-081).
在带有PSMA阳性PC3-PIP瘤的小鼠体内生物分布研究,以评估瘤和骨吸收.
使用加-68 ([68Ga]) 标记的模拟物 ([68Ga]Ga-P17-079) 进行PET成像,以确认体内双重准.

主要成果:

[177Lu]Lu-P17-079和[177Lu]Lu-P17-081都在PSMA阳性瘤中显示出高吸收率,与[177Lu]Lu-PSMA-617相比.
与[177Lu]Lu-PSMA-617相比,[177Lu]Lu-P17-079和[177Lu]Lu-P17-081的骨吸收率显著更高.
[68Ga]Ga-P17-079 PET成像证实了有效的双重向PSMA阳性瘤和骨.

结论:

[177Lu]Lu-P17-079是一种有前途的异质双价放射性核酸治疗剂,具有针对前列腺癌的双重向潜力.
这种药物有效地向表达PSMA的瘤和骨转移,为治疗策略提供了潜在的进步.
对[177Lu]Lu-P17-079的进一步临床前和临床开发对于晚期前列腺癌的治疗是有必要的.

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