Resistance characteristics of sirolimus

Sirolimus (sirolimus) inhibits cell proliferation and induces apoptosis in a dose-dependent manner. Sirolimus (10nmol/L) significantly increases the sensitivity of cells to anti-cancer drugs, resulting in a decrease in the IC50 values of ADM, GEM and MTX. Treatment with sirolimus increased the levels of miR-34b in cells by 7.5-fold. Upregulation of miR-34b also induces apoptosis and increases cellular sensitivity to anticancer drugs.

Sirolimus is the first generationmTOR inhibitor. Sirolimus can also be used as a multidrug resistance reversal agent. Based on several findings, we hypothesized that sirolimus would induce OS cell apoptosis and increase the sensitivity of the OS cell line MG63/ADM. It acts as a gene regulator and controls complex regulatory networks by cleaving or translationally repressing targeted mRNAs. Two new targets of sirolimus were discovered, p21-activated protein kinase 1 (PAK1) and ABCB1/MDR1 gene. The relationship between miR-34b levels and OS prognosis was also evaluated, and drug resistance was found to be closely related to the expression of miR-34b.

SirolimusThe original drug has been launched in China and has entered the scope of Class B medical insurance. SpecificationsThe price of each box of 1mg*10 tablets is about 400 yuan. The domestic drug is only available to patients with anti-rejection reactions in organ transplantation. Patients who do not meet the conditions may not be able to purchase this drug. The original sirolimus drug has also been launched overseas. The price of the Turkish version of Specifications1mg*100 tablets per box is around RMB 2,000 (the price may fluctuate due to exchange rates). The ingredients of the original drugs marketed in China are basically the same as those of foreign original drugs. Currently, there are no generic sirolimus drugs produced in other countries.