Todo S, Porter K A, Kam I, Lynch S, Venkataramanan R, DeWolf A, Starzl T E
Transplantation. 1986 Mar;41(3):296-300. doi: 10.1097/00007890-198603000-00004.
The immunosuppressive qualities and other features of a new cyclosporine (CsA) analogue, Nva2-cyclosporine (Nva2-CsA) were examined using canine orthotopic liver allografts. The mean survival time was 11.8 +/- 9.6 (SD) days in dogs without treatment, 60.8 +/- 4.4 days with Nva2-CsA and 65.1 +/- 33.0 days with CsA. Functional abnormalities indicating toxic side effects were not noted either with Nva2-CsA or with CsA. Using the same oral dose, the rate of blood level rise and the amount of the rise were greater with Nva2-CsA. Histopathologically, Nva2-CsA treatment was associated with the same degree of hydropic vocuolation in the pars recta of the proximal tubules as CsA treatment. Thus, in the dog, Nva2-CsA had identical immunosuppressive properties as CsA, with no functionally detectable toxicity affecting the liver and kidney.
使用犬原位肝同种异体移植研究了一种新型环孢素(CsA)类似物Nva2 - 环孢素(Nva2 - CsA)的免疫抑制特性和其他特征。未治疗的犬的平均存活时间为11.8±9.6(标准差)天,使用Nva2 - CsA的犬为60.8±4.4天,使用CsA的犬为65.1±33.0天。无论是Nva2 - CsA还是CsA,均未观察到表明有毒副作用的功能异常。使用相同的口服剂量时,Nva2 - CsA的血药浓度上升速率和上升量更大。组织病理学上,Nva2 - CsA治疗与CsA治疗在近端小管直部产生的水样空泡化程度相同。因此,在犬中,Nva2 - CsA具有与CsA相同的免疫抑制特性,对肝脏和肾脏没有功能上可检测到的毒性。