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(Sirolimus, SIR) is a new type of immunosuppressant. Studies have proven that the immunosuppressive intensity of rapamycin is better than that of cyclosporine (CsA), which is currently commonly used. After entering the body, the drug binds to FK-binding protein-12 (FKBP-12), inhibits the specific regulatory protein (mTOR), and then blocks the binding of interleukin-2 (IL-2) to its receptor, inhibiting T lymphocytes from entering the S phase from G1 phase, so that Tc and Td cells cannot become sensitized T lymphocytes with immune response.

Rapamin is absorbed quickly, and the time required to reach the maximum blood concentration is 1-2 hours, but the bioavailability F is only about 14%. SIR mainly occurs through demethylation reaction and/or hydroxylation reaction through the hepatocyte microsomal enzyme system CYP3A4 and CYP3A5. Metabolites are mainly excreted through bile and feces, with only 2.2% measured in urine.

Other studies have shown that the in vivo process of rapamycin (i.e. sirolimus) has obvious individual differences, and age, race, diet, genetics, etc. may affect its pharmacokinetic parameters. In order to enable patients to obtain better therapeutic effects, patients must strictly follow the instructions or doctor's instructions to take the medication.

Under normal circumstances, rapamin (sirolimus tablets) is recommended to be used in combination with cyclosporine and corticosteroids. The medication is taken orally once a day. The bioavailability of crushed, chewed, or cut tablets has not been established and such use is not recommended. Patients who cannot take tablets should be prescribed the oral solution and instructed on its use. Patients should start taking sirolimus as soon as possible after transplantation. To minimize differences in sirolimus absorption, the drug should be taken regularly with or without food. Grapefruit juice can slow down the effects of the drug (i.e. sirolimus tablets), so it should not be used to take sirolimus while the patient is taking the drug.

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