Signaling pathway inhibitors of calcineurin-nuclear factor of activated T cells:research progress / 中国药理学与毒理学杂志

Calcineurin (CaN) serves as a key enzyme in human immune regulation. The most important target of this enzyme is the transcription factors of nuclear factors of activated T cells (NFATc). The discovery of the immunosuppressive function of CaN inhibitors (CNIs),ciclosporin A (CsA) and tacrolimus (FK506),has helped overcome the immune rejection of organ transplantion and changed organ transplantion fundamentally. Both of these drugs are still widely used in clinical and basic research,but their therapeutic effects are limited by their serious side effects,including renal tox?icity and neurotoxicity. Therefore,the development of new CNIs with higher specificity and fewer side effects in the clinic is a focus of research. In this paper,the newly discovered and synthesized CNIs in recent decades,including the CsA and FK506 derivatives,direct inhibitors of CaN,as well as the inhibitors that specifically interfere with CaN-NFATc interaction,were summarized.

Influence of CYP3A and MDR1 genetic polymorphisms on the pharmacokinetics of ciclosporin A / 国际药学研究杂志

Ciclosporin A (CsA), an immunosuppressive macrolide antibiotics, is widely applied to prevent rejections after organ transplants. CsA is mainly transported by P-glycoprotein (P-gp) and metabolized by cytochrome P450 (CYP450) 3A.Genetic polymorphisms of CYP3A and MDR1 probably influence the expressions and bioactivity of CYP3A and P-gp,and may affect the pharmacokinetics of CsA.This issue summarizes the correlation between genetic polymorphisms of CYP3A and MDR1 and the pharmacokinetics of CsA to guide the rational and individualized medication.

Influence of CYP3A and MDR1 genetic polymorphisms on the pharmacokinetics of ciclosporin A / 国际药学研究杂志

Ciclosporin A (CsA). an immunosuppressive macrolide antibiotics, is widely applied to prevent rejections after organ transplants. CsA is mainly transported by P-glycoprotein (P-gp) and metabolized by cytochrome P450 (CYP450) 3A.Genetic polymorphisms of CYP3A and MDRl probably influence the expressions and bioactivity of CYP3A and P-gp.and may affect the pharmacokinetics of CsA.This issue summarizes the correlation between genetic polymorphisms of CYP3A and MDRl and the pharmacokinetics of CsA to guide the rational and individualized medication.

Comparative Analysis of Blood Concentrations of Ciclosporin A in Renal Transplant Patients between the Young and Middle-aged Group and the Older-aged Group / 中国药房

60a,24cases)according to their age,the blood concentrations of the2groups in different time were compared.RESULTS:Under the circumstance of close oral dosage of CsA,the blood concentration of CsA in the older-aged group were found remarkably higher than that in the young&middle-aged group(P