ADC 下一代 — 载荷创新
双特异性T细胞衔接器(TCE)一头结合CD3、一头结合肿瘤抗原,把细胞毒性T细胞招募到肿瘤旁,这一模式在B细胞肿瘤中已获充分验证,但毒性始终是绕不开的代价:blinatumomab在复发/难治B细胞淋巴瘤中显示疗效,神经事件却是其剂量限制性毒性[5][6];采用knobs-into-holes技术的全长CD20/CD3双抗则着力改善药代动力学与可制造性[3]。在实体瘤,缺乏足够肿瘤特异性的靶点会带来"on-target off-tumor"毒性,进展明显更慢[4]。DLL3因在小细胞肺癌细胞表面高表达而正常细胞几乎不表达而备受青睐[1];DLL3/CD3双抗tarlatamab的I期研究入组107例患者,≥3级治疗相关不良事件达30.8%,细胞因子释放综合征见于52%的患者,另有1例5级肺炎[2]。如何在维持疗效的同时获得更可控的安全性,是这一领域卡了很久的关口。
在AACR 2026年会上,Y. Liang报告了一款新型DLL3三特异性T细胞衔接器抗体:在DLL3与CD3之外,它整合了CD2/CD58共刺激通路,摘要标题给出的结论是"更优的抗肿瘤疗效与均衡的安全性"(会议摘要编号4046)[7]。同一条消息还指向JITC的一项研究(14卷2期,e013986),称三特异性TCE设计正在推动多发性骨髓瘤的治疗。需要留意的是,DLL3的主要研究背景是小细胞肺癌等神经内分泌肿瘤[1],与骨髓瘤并不重合,这层关联的确切含义有待原文献说明。
这一设计的推进之处,在于把共刺激信号直接写进衔接器。既往研究显示,作为CD2共刺激受体配体的CD58在肿瘤中频繁发生改变,其丢失会降低TCE介导的细胞毒性并介导对BiTE治疗的内在耐药[8],为纳入CD2/CD58通路提供了理论动机;技术路线上,Mikami等曾将CD3/CD137双重特异性引入DLL3衔接器,观察到更好的肿瘤生长控制和瘤内T细胞数量增加[9],本次改用CD2/CD58,可视为同一方向上的新变体。临床端的同类布局也在推进:靶向CD3/DLL3/DLL3的三特异性衔接器ZG006已进入治疗复发难治小细胞肺癌或神经内分泌癌的I期剂量递增与扩展研究[10],说明三特异性形态已开始接受人体检验。
不过,目前可见的仅是摘要标题层面的信息,支持“更优疗效与均衡安全性”的具体数据、模型与样本量均未披露;对比tarlatamab 52%的CRS发生率[2],这类设计能否在人体中真正兑现安全性优势,仍需完整报告和临床试验回答;它与消息中提及的骨髓瘤JITC研究之间的实际关系,同样有待读到全文才能判断。
- 1.Emerging therapies targeting the delta-like ligand 3 (DLL3) in small cell lung cancer · J Hematol Oncol 2023
- 2.Tarlatamab, a First-in-Class DLL3-Targeted Bispecific T-Cell Engager, in Recurrent Small-Cell Lung Cancer: An Open-Label, Phase I Study · J Clin Oncol 2023
- 3.Anti-CD20/CD3 T cell-dependent bispecific antibody for the treatment of B cell malignancies · Sci Transl Med 2015
- 4.An anti-glypican 3/CD3 bispecific T cell-redirecting antibody for treatment of solid tumors · Sci Transl Med 2017
- 5.Phase 2 study of the bispecific T-cell engager (BiTE) antibody blinatumomab in relapsed/refractory diffuse large B-cell lymphoma · Blood 2016
- 6.Bispecific T-Cell Engager (BiTE) Antibody Construct Blinatumomab for the Treatment of Patients With Relapsed/Refractory Non-Hodgkin Lymphoma: Final Results From a Phase I Study · J Clin Oncol 2016
- 7.Abstract 4046: A novel DLL3 trispecific T cell engager ... · aacrjournals.org 2026
- 8.intrinsic resistance to BiTE therapy is mediated by loss of ... · jitc.bmj.com 2026
- 9.Engineering CD3/CD137 Dual Specificity into a DLL3- ... · pubmed.ncbi.nlm.nih.gov 2026
- 10.A phase 1 dose escalation and expansion study of ZG006 ... · asco.org 2026
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@SawyersLabMSKCC
. NOTCH and YAP/TAZ seem to restrain NE lineage transformation and enrich for NE-low states - could TEADi promote response to DLL3 therapies in NECs?
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Rohit Thummalapalli, Ming Lu, Alexander Spira, Amr Mohamed, Rahul Aggarwal, Yu Wang, Namrata Vijayvergia, Jordi Rodon, Andrew Scott Paulson, Pingkuan Zhang, Hui Yang, Yuan Xin, Jingmin Wen, Jie Chen
Read the abstract →Source: Rohit Thummalapalli · x.com
