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雷帕鸣是治疗什么病症的药?

Author: Medicalhalo
Release time: 2025-10-19 11:44:20

It was approved by the FDA on May 30, 2007 for the treatment of advanced renal disease. It has now entered clinical phase 4 for the treatment of mantle cell lymphoma. Rapamycin is an inhibitor of the rapamycin target protein mTOR. mTOR is a downstream protein of the PI3K/AKT pathway. This pathway is abnormally activated in a variety of tumor cells. It can control the growth of tumor cells by inhibiting the activity of mTOR and thereby inhibiting the activity of its downstream S6 ribosomal protein kinase (S6K1). In addition, rapamycin also has its own activity and can be converted into rapamycin in the body to inhibit mTOR.  

Sirolomus, formerly known as Rapamycin Rapamune (RPM), is a lipophilic triene nitrogen-containing macrolide antibiotic immunosuppressive drug produced by Streptomyces hygroscopieus isolated from soil samples of Easier Island in the Pacific by Vezina and others at Ayerst Laboratory in Canada in 1975. In 1989, Morris officially began to study RPM as a new highly effective immunosuppressant for anti-rejection of organ transplantation. The effective anti-proliferative effect on peripheral blood mononuclear cells was found to be 50 to 500 times stronger than that of cyclosporine CA. Less nephrotoxic than cyclosporine and tacrolimus. Used in combination with cyclosporine to produce a synergistic effect. Although rapamycin is structurally homologous to TRL (Tacmlimus, FK506) and binds to the same immune-binding protein, their mechanisms of action are different. SRL inhibits the activity and proliferation of T cells and also inhibits the production of antibodies. In cells, SRL combines with the immunosuppressive protein FKBP 12 to produce an immunosuppressive complex. The SLR:FKBP 12 complex, which has no effect on calmodulin, binds to the rapamycin target site in mammalian cells and inhibits its activation. This inhibitory effect inhibits lymphokine-driven T cell proliferation and inhibits the progression from G1 to S phase in T cell evolution and differentiation. As a novel potent immunosuppressant with low toxicity, it can prolong the survival period after transplantation, reduce the occurrence of acute rejection, and provide a new treatment alternative for transplant recipients.

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