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编 号:F323208
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CAS No: 332348-12-6
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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 human IgG1 (hinge and CH2 and 3 domains). Abatacept is a selective T-cell co-stimulation modulator and a protein agent for the autoimmune diseases.
体内研究:
与静脉给药组相比,Abatacept 减轻了爪水肿,皮下注射多剂量组的爪水肿明显减少 (tobs=2.50)。 Abatacept 在研究剂量范围内表现出线性 PK。NCA 清除率 (CL) 为 20.8 mL/day/kg,容积 (Vss) 为 146 mL/kg,皮下给药的生物利用度 (F) 为 57.7%。 Abatacept (口服;10 mg/kg;每 2 天一次) 降低活化 T 细胞 (CD44highCD62L–) 的比例并抑制纯合子 DO11.10 RAG-2 中 ICOS 和 CD71 的上调–/– BALB/c (H-2d/d) 小鼠。Animal Model:Male Lewis rats (6-9 weeks old) with weights of 150-175 g
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
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%.