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开发,特征和辐射剂量测量研究F-BMS-986229,一个F-标记PD-L1宏环PET标记仪
Joonyoung Kim1, David J Donnelly2, Tritin Tran2
1Bristol Myers Squibb Research and Early Development, P.O. Box 4000, Princeton, NJ, 08543, USA. joonyoung.kim@bms.com.
Molecular imaging and biology
|December 20, 2023
概括
一种新的F-标记的标记器,F-BMS-986229,可以准确,定量评估被编程的死亡配体1 (PD-L1) 表达. 这种PET追踪器对监测癌症患者免疫疗法反应有前途.
科学领域:
- 核医学就是核医学.
- 在瘤学瘤学.
- 放射化学 放射化学是指辐射化学.
背景情况:
- 针对编程死亡-1 (PD-1) 和编程死亡-连接体1 (PD-L1) 相互作用的癌症免疫疗法是一个有希望的策略.
- 对PD-1/PD-L1抑制的耐药性可能来自可变的瘤细胞PD-L1表达,需要超越标准免疫组织化学 (IHC) 的高级定量评估.
- 需要一种全面和定量方法来测量PD-L1表达,以改善治疗策略.
研究的目的:
- 开发和描述一种新的F标记的宏环标记器,用于正子发射断层扫描 (PET) 成像.
- 评估追踪器在癌症患者中全面评估瘤PD-L1表达的能力.
- 调查追踪器在监测纵向变化和预测免疫治疗结果方面的潜力.
主要方法:
- 使用体外和体外自发放射学进行F-BMS-986229的表征.
- 在小鼠体内进行PET成像,以评估标记物吸收和与PD-L1抑制剂的向接触 (BMS-986189).
- 在健康的非人类灵长类动物 (NHPs) 中对F-BMS-986229进行全身辐射剂量测试.
主要成果:
- 在体外自射成像显示了对PD-L1表达瘤的高结合特异性 (8:1比).
- 在小鼠体内PET成像显示,PD-L1阳性瘤具有高特异性结合 (>83%) 的显著标志物吸收.
- 在NHP的剂量测试研究表明,低全身有效剂量 (0.025 mSv/MBq),支持临床适用性.
结论:
- F-BMS-986229已在临床前验证为具有高目标特异性和低背景吸收的PET追踪剂.
- 追踪器的短血半衰期允许在同一天进行成像,从而促进临床使用.
- 在癌症免疫治疗中,F-BMS-986229显示了量化PD-L1表达和监测治疗反应的显著潜力.
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