雷帕鸣和雷帕霉素有什么区别

Sirolimus (sirolimus), also known as rapamycin, is a macrolide antibiotic immunosuppressant. Its chemical structure is similar to tacrolimus, but its mechanism of action is different. Although both bind to FK-binding protein (FKBP12), the RAPA-FKBP12 complex does not act on calcineurin but on the mammalian target of rapamycin (mTor). mTOR promotes the growth of T cells by initiating and promoting the transcription process to synthesize new proteins, and its point of action is in the late stages of T cell activation, that is, the G1 to S phase.

Unlike tacrolimus, sirolimus cannot inhibit the secretion of important cytokines in the early stages of T cell activation, but it can block the activation of calcium ion-dependent and calcium ion-independent T cells. It can also regulate the proliferation, activation and antibody secretion of B lymphocytes. In addition, sirolimus can also inhibit the proliferation of non-immune cells. It inhibits the proliferation of fibroblasts, endothelial cells, hepatocytes and smooth muscle cells by inhibiting the secretion of fibroblast growth factor, platelet-derived growth factor, endothelial cell growth factor and transforming growth factor.

As a new type of immunosuppressant, since it was approved by the FDA for clinical kidney transplantation in 1999, while rapamycin exerts an immunosuppressive effect, it has many advantages such as low nephrotoxicity, few side effects, and anti-tumor. In particular, its potential in inducing immune tolerance after transplantation has quickly attracted everyone's attention. Most current experimental studies have confirmed that sirolimus plays a role in inducing and maintaining immune tolerance, mainly through its effects on T cells and dendritic cells, which can significantly increase the number of antigen-specific inducible regulatory T cells.

It is best for patients to use it under the guidance of a clinician during treatment. Because blind use of medication may have some unsafe factors, patients should use it according to the doctor's recommendations.

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