Abatacept (CTLA4lg) 是一种可溶性融合蛋白，由人 CTLA4 的胞外结构域和人 IgG1 Fc 部分的片段 (铰链，CH2 和 3 结构域) 组成。Abatacept 是选择性 T 细胞共刺激调节剂，也是一种用于自身免疫性疾病的蛋白药物。
| 生物活性 | Abatacept (CTLA4lg) is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of humanIgG1(hinge and CH2 and 3 domains)[1]. Abatacept is a selective T-cell co-stimulation modulator and a protein drug for the autoimmune diseases[2]. |
体内研究
(In Vivo) | Abatacept reduces paw edema, and the SC Multiple-dose group shows significantly greater (tobs= 2.50) paw edema reduction compared with the IV dose group[2].
Abatacept exhibits linear PK across the studied doses. The NCA clearance (CL) is 20.8 mL/day/kg, volume (Vss) is 146 mL/kg, and bioavailability (F) of the SC dose dosing is 57.7%[2].
Abatacept (oral; 10 mg/kg; every 2 days) reduces the proportion of activated T cells (CD44highCD62L–) and inhibits the up-regulation of ICOS and CD71 in homozygous DO11.10 RAG-2–/–BALB/c (H-2d/d) mice[3].
| Animal Model: | Male Lewis rats (6-9 weeks old) with weights of 150-175 g[2] | | Dosage: | 10 mg/kg (IV), 20 mg/kg (SC single-dose), 20 mg/kg (SC Multiple-dose) on day 21 with 10 mg/kg SC doses on days 23, 25, 27, and 29 | | Administration: | IV or SC | | Result: | Reduced paw edema, and the SC Multiple-dose group showed significantly greater (tobs= 2.50) paw edema reduction compared with the IV dose group. |
| Animal Model: | Male Lewis rats (6-9 weeks old) with weights of 150-175 g[2] | | Dosage: | 10 mg/kg (IV), 20 mg/kg (SC single-dose), 20 mg/kg (SC Multiple-dose) on day 21 with 10 mg/kg SC doses on days 23, 25, 27, and 29 (Pharmacokinetic Study) | | Administration: | IV or SC | | Result: | The NCA clearance (CL) is 20.8 mL/day/kg, volume (Vss) is 146 mL/kg, and bioavailability (F) of the SC dose dosing is 57.7%. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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