Vobarilizumab

Vobarilizumab (ALX-0061) is an anti-IL-6R monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis[1][2][3].

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related

Research Areas >> Inflammation/Immunology

Vobarilizumab 显示出对 sIL-6R 的优先结合亲和力 (与 mIL-6R 相比) [2]。 Vobarilizumab (0-10 nM) 阻断重组 hIL-6 与重组 hsIL-6R 的相互作用[3]。 Vobarilizumab (0-100 nM) 可抑制 TF-1 细胞的增殖[3]。

Vobarilizumab (0.4-10 mg/kg，静脉注射) 抑制食蟹猴中 hIL-6 诱导的炎症[3]。 Vobarilizumab (0.4-10 mg/kg，静脉注射) 通过与食蟹猴的血清白蛋白结合显示出长期暴露[3]。 Animal Model: hIL-6-induced inflammation in cynomolgus monkey[3] Dosage: 0.4 mg/kg, 2 mg/kg, or 10 mg/kg Administration: Intravenous injection (i.v.) Result: Inhibited the acute phase response parameters: plasma levels of C-reactive protein (CRP), fibrinogen and platelets. Animal Model: Cynomolgus monkeys[3] Dosage: 0.4 mg/kg, 2 mg/kg, or 10 mg/kg Administration: Intravenous injection (i.v.) Result: Pharmacokinetic parameters of Vobarilizumab dose (mg/kg) T1/2 dominant (day) AUCinf (μg/day/mL) CL (mL/day/kg) Vss (mL/kg) 0.4 (i.v.) 1.73 16.3 24.8 42.8 2 (i.v.) 5.0 193 10.4 53.7 10 (i.v.) 6.61 1136 9 82.7

[1]. Kerschbaumer A, et al. Efficacy of pharmacological treatment in rheumatoid arthritis: a systematic literature research informing the 2019 update of the EULAR recommendations for management of rheumatoid arthritis. Ann Rheum Dis. 2020 Jun;79(6):744-759.  

[2]. M. Van Roy, et al. FRI0021 Alx-0061, an anti-IL-6r nanobody® for therapeutic use in rheumatoid arthritis, demonstrates in vitro a differential biological activity profile as compared to tocilizumab. Ann Rheum Dis. 2013. 72 (3).

[3]. Van Roy M, et al. The preclinical pharmacology of the high affinity anti-IL-6R Nanobody® ALX-0061 supports its clinical development in rheumatoid arthritis. Arthritis Res Ther. 2015 May 20;17(1):135.