Sirolimus Capsules

Sirolimus inhibits the activation and proliferation of T lymphocytes stimulated by antigens and cytokines (interleukins IL-2, IL-4 and IL-15) through a mechanism of action that is completely different from other immunosuppressants. Sirolimus also inhibits the production of antibodies. In cells, sirolimus binds to the immunophilin, FK binding protein-12 (FKBP-12), to form an immunosuppressive complex. This sirolimus FKBP-12 complex has no effect on the activity of calcineurin. This complex binds to the mammalian target of sirolimus (mTOR, a key regulatory kinase) and inhibits its activity. This inhibition blocks the proliferation of cytokine-driven T cells, that is, inhibits the progression from the G1 phase to the S phase of the cell cycle. Experimental model studies have shown that sirolimus can prolong the survival of allogeneic transplants (kidney, heart, skin, pancreatic islets, small intestine, pancreato-duodenal and bone marrow) in mice, rats, pigs and/or primates. Sirolimus reverses acute rejection of cardiac and renal allografts in rats and prolongs graft survival in presensitized rats. In some studies, the immunosuppressive effects of sirolimus persist for up to 6 months after cessation of treatment. This immune tolerance effect is alloantigen specific. In rodent models of autoimmune disease, sirolimus inhibits immune-mediated responses associated with systemic lupus erythematosus, collagen-induced arthritis, autoimmune type I diabetes, autoimmune myocarditis, experimental allergic encephalomyelitis, graft-versus-host disease, and autoimmune uveoretinitis.

Molecular weight: C51H79NO13

This product is in the form of capsules.

For patients who have received a kidney transplant to prevent organ rejection

oral.

Very common (according to the International Council of Medical Organizations frequency classification, the incidence is 10%): lymphocele, peripheral edema, abdominal pain, diarrhea, hypokalemia, increased lactate dehydrogenase, acne, urinary tract infection; very common at higher doses: anemia, hypercholesterolemia, thrombocytopenia, hypertriglyceridemia (hyperlipidemia). Store in a cool, dry, dark environment.

It is contraindicated in patients who are allergic to sirolimus, its derivatives, or any ingredients in the oral solution of this medicine, as well as in pregnant and lactating women.

Precautions for children: The safety and efficacy of this drug for pediatric patients under 13 years old have not been determined. When using this drug in pediatric patients under 13 years old, blood trough concentrations should be monitored. Precautions for pregnancy and lactation: Pregnant and lactating women are prohibited. Precautions for the elderly: In the clinical trials of this drug, there were not enough cases of patients aged 65 and above to determine whether the safety and efficacy of this population differ from those of younger patients. The data on the trough concentration of sirolimus indicate that the dose of this drug does not need to be adjusted according to age for elderly patients with kidney disease.

Sirolimus is known to be a substrate of cytochrome CYP3A4 and P-glycoprotein. The pharmacokinetic interactions of sirolimus and some drugs when taken simultaneously are as follows. The interaction with other drugs has not been studied.

Keep away from light and store in sealed container.

0.5mg

24 months

North China Pharmaceutical Company.Ltd

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