Tietz Julia, Gunde Tea, Warmuth Stefan, Weinert Christopher, Brock Matthias, Simonin Alexandre, Hess Christian, Johansson Maria, Spiga Fabio, Muntwiler Simone, Wickihalder Belinda, Mahler Dana, Diem Dania, Zeberer Julia, Heiz Robin, Flückiger Naomi, Shiraishi Noriko, Miyake Yoshihide, Takahashi Nobuaki, Fehrholz Markus, Bertolini Marta, Lichtlen Peter, Urech David, Snell Daniel
Numab Therapeutics AG, Zürich, Switzerland.
Kaken Pharmaceutical, Tokyo, Japan.
JID Innov. 2024 Jan 16;4(2):100258. doi: 10.1016/j.xjidi.2024.100258. eCollection 2024 Mar.
Inhibition of IL-4/IL-13 signaling has dramatically improved the treatment of atopic dermatitis (AD). However, in many patients, clinical responses are slow to develop and remain modest. Indeed, some symptoms of AD are dependent on IL-31, which is only partially reduced by IL-4/IL-13 inhibition. Thus, there is an unmet need for AD treatments that concomitantly block IL-4/IL-13 and IL-31 pathways. We engineered NM26-2198, a bispecific tetravalent antibody designed to accomplish this task. In reporter cell lines, NM26-2198 concomitantly inhibited IL-4/IL-13 and IL-31 signaling with a potency comparable with that of the combination of an anti-IL-4Rα antibody (dupilumab) and an anti-IL-31 antibody (BMS-981164). In human PBMCs, NM26-2198 inhibited IL-4-induced upregulation of CD23, demonstrating functional binding to FcγRII (CD32). NM26-2198 also inhibited the secretion of the AD biomarker thymus and activation-regulated chemokine (TARC) in blood samples from healthy human donors. In male cynomolgus monkeys, NM26-2198 exhibited favorable pharmacokinetics and significantly inhibited IL-31-induced scratching at a dose of 30 mg/kg. In a repeat-dose, good laboratory practice toxicology study in cynomolgus monkeys, no adverse effects of NM26-2198 were observed at a weekly dose of 125 mg/kg. Together, these results justify the clinical investigation of NM26-2198 as a treatment for moderate-to-severe AD.
抑制IL-4/IL-13信号通路已显著改善了特应性皮炎(AD)的治疗效果。然而,在许多患者中,临床反应出现缓慢且效果仍较为有限。实际上,AD的某些症状依赖于IL-31,而IL-4/IL-13抑制只能部分降低其水平。因此,对于能同时阻断IL-4/IL-13和IL-31通路的AD治疗方法仍存在未满足的需求。我们构建了NM26-2198,一种旨在完成此任务的双特异性四价抗体。在报告细胞系中,NM26-2198能同时抑制IL-4/IL-13和IL-31信号通路,其效力与抗IL-4Rα抗体(度普利尤单抗)和抗IL-31抗体(BMS-981164)联合使用时相当。在人外周血单核细胞中,NM26-2198抑制IL-4诱导的CD23上调,表明其与FcγRII(CD32)具有功能性结合。NM26-2198还抑制了健康人类供体血样中AD生物标志物胸腺和活化调节趋化因子(TARC)的分泌。在雄性食蟹猴中,NM26-2198表现出良好的药代动力学特性,在30 mg/kg的剂量下能显著抑制IL-31诱导的抓挠行为。在一项食蟹猴重复给药的良好实验室规范毒理学研究中,每周剂量为125 mg/kg时未观察到NM26-2198有任何不良反应。综上所述,这些结果证明了对NM26-2198作为中重度AD治疗方法进行临床研究的合理性。