雷帕鸣是雷帕霉素吗

(sirolimus) is a mammalian target of rapamycin (mTORi) inhibitor. It is a macrolide antibiotic isolated from the culture medium of actinomycetes. It was originally developed as an antifungal drug, but it has anti-cancer activity (high dose) and immunosuppressive effects in mouse models. These effects are not conducive to anti-infection but beneficial to transplantation. In 1999, sirolimus was approved as a maintenance immunosuppressant, and experimental models of renal cell carcinoma confirmed its significant anti-tumor effect.

In in vitro tests, rapamycin (sirolimus) can convert rat renal cancer cells from invasive to non-invasive, strengthen the connection of E-cadherin between cells, thereby reducing the spread and metastasis of cancer cells, reduce cancer cell cycle protein D1 and increase P27 key intermediate protein-1, inhibit the transition of cancer cells from G1 phase to S phase, thereby slowing down the growth of tumors.

In several mouse renal cell carcinoma progression models, sirolimus inhibited tumor growth and metastasis and prolonged survival even after induction with cyclosporine. In the SCLD-mouse model of human renal cell carcinoma lung metastasis, sirolimus showed anti-tumor efficacy by specifically reducing the tumor-promoting cytokines TGFβ and VEGF-A. Compared with cyclosporine, sirolimus has anti-angiogenic effects and can indirectly produce anti-tumor effects by down-regulating VEGF and anti-angiogenic effects. It also has an inhibitory effect on abnormally active upstream molecules. Everolimus exerts an anti-B lymphocyte proliferation effect by reducing the secretion of IL-10, which suggests that it has the potential to prevent or treat PTLD.

Because it has the advantages of non-nephrotoxicity, anti-tumor, and can reduce the incidence of cytomegalovirus infection, it has attracted clinical attention and been widely used. Currently, there are two main clinical strategies for using sirolimus: initial use of sirolimus (without calcineurin inhibitors) after kidney transplantation, and switching from calcineurin inhibitor drugs to sirolimus after kidney transplantation.

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