Department of Internal Medicine II, University Hospital of Würzburg, Würzburg.
Department of Ophthalmology, University Hospital of Würzburg, Würzburg.
Haematologica. 2024 Nov 1;109(11):3670-3680. doi: 10.3324/haematol.2024.285205.
Belantamab mafodotin (belantamab) is a first-in-class anti-B-cell maturation antigen (BCMA) antibody-drug conjugate approved for the treatment of triple-class refractory multiple myeloma. It provides a unique therapeutic option for patients ineligible for chimeric antigen receptor (CAR) T and bispecific antibody therapy, and/or patients progressing on anti-CD38 treatment where CAR T and bispecifics might be kept in reserve. Wider use of the drug can be challenged by its distinct ocular side effect profile, including corneal microcysts and keratopathy. While dose reduction has been the most effective way to reduce these toxicities, the underlying mechanism of this BCMA off-target effect remains to be characterized. In this study, we provide the first evidence for soluble BCMA (sBCMA) in lacrimal fluid and report on its correlation with tumor burden in myeloma patients. We confirm that corneal cells do not express BCMA, and show that sBCMA-belantamab complexes may rather be internalized by corneal epithelial cells through receptor-ligand independent pinocytosis. Using an hTcEpi corneal cell-line model, we show that the pinocytosis inhibitor EIPA significantly reduces belantamab-specific cell killing. As a proof of concept, we provide detailed patient profiles demonstrating that, after belantamab-induced cell killing, sBCMA is released into circulation, followed by a delayed increase of sBCMA in the tear fluid and subsequent onset of keratopathy. Based on the proposed mechanism, pinocytosis-induced keratopathy can be prevented by lowering the entry of sBCMA into the lacrimal fluid. Future therapeutic concepts may therefore consist of belantamab-free debulking therapy prior to belantamab consolidation and/or concomitant use of γ-secretase inhibition as currently evaluated for belantamab and nirogacestat in ongoing studies.
贝兰他单抗(belantamab)是一种首创的抗 B 细胞成熟抗原(BCMA)抗体药物偶联物,已被批准用于治疗三药难治性多发性骨髓瘤。对于不适合嵌合抗原受体(CAR)T 和双特异性抗体治疗的患者,以及/或接受抗 CD38 治疗后可能保留 CAR T 和双特异性药物的患者,它提供了一种独特的治疗选择。由于其独特的眼部副作用谱,包括角膜微囊和角膜病,该药的广泛应用可能受到挑战。虽然减少剂量是减少这些毒性最有效的方法,但这种 BCMA 脱靶效应的潜在机制仍有待阐明。在这项研究中,我们首次提供了泪液中可溶性 BCMA(sBCMA)的证据,并报告了其与骨髓瘤患者肿瘤负担的相关性。我们证实角膜细胞不表达 BCMA,并表明 sBCMA-贝兰他单抗复合物可能通过受体-配体非依赖性胞吞作用被角膜上皮细胞内化。使用 hTcEpi 角膜细胞系模型,我们表明,胞吞抑制剂 EIPA 可显著减少贝兰他单抗特异性细胞杀伤。作为概念验证,我们提供了详细的患者概况,表明在贝兰他单抗诱导的细胞杀伤后,sBCMA 被释放到循环中,随后在泪液中 sBCMA 延迟增加,并随后出现角膜病。基于提出的机制,通过降低 sBCMA 进入泪液的量,可以预防胞吞作用引起的角膜病。因此,未来的治疗概念可能包括在贝兰他单抗巩固治疗之前进行无贝兰他单抗的减瘤治疗,和/或在正在进行的研究中,像目前对贝兰他单抗和尼洛替尼评估的那样,同时使用 γ-分泌酶抑制。