sirolimus治疗肾移植效果如何？

The main ingredient is sirolimus, formerly known as rapamycin, which is a new type of powerful lipophilic triene nitrogen-containing macrolide antibiotic immunosuppressant. As a third-generation immunosuppressant, its anti-proliferative effect on peripheral blood mononuclear cells is 50-500 times stronger than that of cyclosporine. Due to its low nephrotoxicity, American Home Products Company (AHP) was officially approved by the FDA in September 1999 as an anti-rejection drug for kidney transplantation. At the same time, it has a variety of activities that have attracted the attention of experts in various fields. It has anti-tumor activity alone or/in combination with streptolytic bacteria, has anti-fungal activity, and is a macrolide antibiotic drug with pleiotropic effects on multiple sclerosis.

Sirolimus is indicated for patients undergoing kidney transplantation to prevent organ rejection and is recommended for use in combination with cyclosporine and corticosteroids.

Medication during lactation: Sirolimus is secreted in trace amounts in the milk of lactating rats. It is unknown whether sirolimus is excreted in human milk. The pharmacokinetics and behavior of sirolimus in infants are unclear. Considering that many drugs are excreted in human milk and the potential adverse effects of sirolimus on nursing infants, the decision to discontinue breastfeeding or discontinue the drug should be based on the importance of the drug to the mother.

The main component of sirolimus is sirolimus. Sirolimus inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukins IL-2, IL-4 and IL-15). It also inhibits the production of antibodies. In cells, in clinical trials, a loading dose of 15 mg and a maintenance dose of 5 mg/day were used, but for kidney transplant patients, the efficacy benefit of doses above 2 mg is unclear. Concomitant use with cyclosporine and corticosteroids is recommended for patients taking daily sirolimus. Patients taking sirolimus (Rapamune) 2 mg daily had overall better health than those taking sirolimus (Rapamune) 5 mg daily.

Binds to the immunophilin, FK-binding protein-12 (FKBP-12), to generate the FKBP-12 immunosuppressive complex. This complex binds to the mammalian sirolimus BA molecule (mTOR, a key regulatory kinase) and inhibits its activity, thereby inhibiting the progression from G1 to S phase in the cell cycle.

In clinical trials, a loading dose of 15 mg and a maintenance dose of 5 mg/day were used, but for kidney transplant patients, the therapeutic benefit of doses above 2 mg is unclear. Concomitant use with cyclosporine and corticosteroids is recommended for patients taking daily sirolimus. Patients taking sirolimus (Rapamune) 2 mg daily had overall better outcomes than those taking sirolimus (Rapamune) 5 mg daily.

It can be seen that the treatment effect is still good, and patients can use it with confidence.