Tacrolimus(FK506)is the most widely utilized calcineurin inhibitors(CNIs)and serves as the first-line agent in immunosuppressive treatment regimens.FK506 has a narrow therapeutic index,and its pharmacokinetics exhibit significant vari-ability both between and within individuals.High-dose exposure to FK506,whether administered long-term or short-term,can result in nephrotoxicity.Proximal tubule cells in kidney are the only cells that are capable of metabolizing CNIs,and these cells are believed to play a central role in the development of toxicity associated with this class of drugs.The mechanism underlying renal tubular toxicity induced by FK 506 is complex,involving factors such as cellular oxidative stress,inflammatory responses,metabolic dysfunction of renal tubular cells,apoptosis,and the renin-angiotensin system.Despite extensive research,the patho-genesis of FK506-induced tubular toxicity remains incompletely understood.Therefore,this article aims to review the research progress concerning the pathogenesis of tacrolimus-related renal tubular toxicity,as well as its prevention and treatment,to pro-vide a reference for clinical practice and future research.

Tacrolimus(FK506)is the most widely utilized calcineurin inhibitors(CNIs)and serves as the first-line agent in immunosuppressive treatment regimens.FK506 has a narrow therapeutic index,and its pharmacokinetics exhibit significant vari-ability both between and within individuals.High-dose exposure to FK506,whether administered long-term or short-term,can result in nephrotoxicity.Proximal tubule cells in kidney are the only cells that are capable of metabolizing CNIs,and these cells are believed to play a central role in the development of toxicity associated with this class of drugs.The mechanism underlying renal tubular toxicity induced by FK 506 is complex,involving factors such as cellular oxidative stress,inflammatory responses,metabolic dysfunction of renal tubular cells,apoptosis,and the renin-angiotensin system.Despite extensive research,the patho-genesis of FK506-induced tubular toxicity remains incompletely understood.Therefore,this article aims to review the research progress concerning the pathogenesis of tacrolimus-related renal tubular toxicity,as well as its prevention and treatment,to pro-vide a reference for clinical practice and future research.