Cudarolimab,2244739-29-3

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Cudarolimab

CAS No. : 2244739-29-3

MCE 国际站：Cudarolimab

产品活性：Cudarolimab (IBI101) 是一种完全人抗 OX40 (CD134，一种由激活的免疫细胞表达的共刺激分子) 抗体。Cudarolimab 抑制 OX40 与其配体 OX40L 的结合。Cudarolimab 具有抗肿瘤活性，可用于癌症相关研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Orexin Receptor (OX Receptor)

In Vitro: Cudarolimab (0.01, 1, 100 or 10000 nM) binds to OX40 and partially blocks the binding of OX40 to its ligand OX40L in CHO-S cells overexpressing human OX40 (CHO-S-hOX40). Cudarolimab activates OX40 dependent NF-κB reporters with an EC₅₀ value of 4.432 nM in Jurkat-OX40 reporter cells co-cultured with Raji cells.
Cudarolimab (0.01, 0.1, 1, 10, 100 or 1000 nM) binds to activated human CD4⁺ T cells and activated cynomolgus monkey CD4⁺ T cells in a dose dependent manner.
Cudarolimab (0.4, 4.0 and 40.4 nM) increases IL-2 secretion with dose dependent manner in human CD4⁺ T cells.

In Vivo: Cudarolimab (10 mg/kg; i.p.; single dose on days 3, 7, 11, 14 and 15) significantly reduces tumor volume in humanized NOG mice bearing LoVo tumors.
Cudarolimab (0.1, 1 and 10 mg/kg; i.p.; single dose on days 6, 9, 12 and 16) significantly reduces tumor volume, increases IFN-γ⁺ and IFN-α⁺ expression in CD8⁺ T cells in tumor and spleen of human OX40 knock-in mice bearing MC38 tumors.
Cudarolimab (10 mg/kg; i.p.; single dose on days 10 and 14) significantly reduces the expression of CD3⁺CD8⁺, CD3⁺CD4⁺, CD4⁺CD25^highFoxP3⁺ in the tumor and spleen of human OX40 knock-in mice bearing MC38 tumors.
Pharmacokinetic (PK) parameters of Cudarolimab in cynomolgus macaques

Dose (mg/kg)	Cmax (µg/mL )	Tmax (h)	AUC0-∞ (h•µg/mL )	T1/2 (h)	Cl (mL/h/kg)	MRTlast (h)
0.1	3.07±0.40	0.08±0.00	347.98±99.30	162.98±103.01	0.31±0.08	186.34±110.68
0.5	9.78±3.27	0.40±0.78	1429.19±607.21	129.47±114.44	0.40±0.14	136.03±108.05
2.5	63.10±15.29	0.08±0.00	10304.06±3403.59	190.89±92.94	0.27±0.09	212.29±114.61
12.5	296.57±58.05	0.40±0.78	33511.65±14982.36	120.30±153.26	0.44±0.20	114.93±87.66

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