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Bleselumab

Names

[ CAS No. ]:
1453067-91-8

[ Name ]:
Bleselumab

Biological Activity

[Description]:

Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd:  0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[Target]

CD40[1]


[In Vitro]

Bleselumab (0-1 μg/mL,48 h) 剂量依赖性地抑制可溶性 CD154 诱导的 PBMCs 增殖[2]。 Cell Viability Assay[2] Cell Line: PBMCs Concentration: 0-1 μg/mL Incubation Time: 48 h Result: Inhibited PBMC proliferation induced by shCD154 in human, cynomolgus monkey and rabbit blood samples.

[In Vivo]

Bleselumab (0.1-10mg/kg,静脉注射) 抑制食蟹猴的迟发型超敏反应 (DTH)[2]。 Bleselumab (2 mg/kg,静脉注射) 可延长食蟹猴移植肾的存活时间[3]。 Bleselumab (2 或 5 mg/kg,静脉注射) 与 Tacrolimus (HY-13756) 联用显示比单一疗法更长的中位生存时间 (MST)[3]。 Animal Model: Cynomolgus monkeys[2]. Dosage: 0.1, 1 and 10 mg/kg Administration: Intravenous injection (i.v.) Result: Inhibited anti-TTx IgG and anti-TTx IgM productions in a concentration-dependent manner.

[References]

[1]. Harland RC, et al. Efficacy and safety of bleselumab in kidney transplant recipients: A phase 2, randomized, open-label, noninferiority study. Am J Transplant. 2020 Jan;20(1):159-171.  

[2]. Okimura K, et al. Characterization of ASKP1240, a fully human antibody targeting human CD40 with potent immunosuppressive effects. Am J Transplant. 2014 Jun;14(6):1290-9.  

[3]. Song L, et al. Effects of ASKP1240 combined with tacrolimus or mycophenolate mofetil on renal allograft survival in Cynomolgus monkeys. Transplantation. 2014 Aug 15;98(3):267-76.  

Chemical & Physical Properties

No Any Chemical & Physical Properties


Related Compounds

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