Drug intelligence / Profile preview

cyclosporine + sirolimus + corticosteroids

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cyclosporine + sirolimus + corticosteroids is a combination immunosuppressive regimen primarily used to prevent organ transplant rejection, especially in renal transplantation. Cyclosporine is a calcineurin inhibitor that suppresses T-cell activation by inhibiting interleukin 2 (IL-2) production. Sirolimus (also known as rapamycin) is an mTOR inhibitor that blocks cytokine-driven T-cell proliferation by binding to FKBP12 and inhibiting the mammalian target of rapamycin, thereby preventing cell cycle progression from G1 to S phase. Corticosteroids are anti-inflammatory agents that broadly suppress immune responses through multiple mechanisms, including inhibition of cytokine gene expression and induction of lymphocyte apoptosis. This triple-drug regimen reduces the risk of acute allograft rejection more effectively than dual therapy and is standard in early post-transplant management for patients at moderate or high immunologic risk[1][5][6][7]. The combination may also be used in other immune-mediated conditions such as refractory minimal change nephropathy[3].

Other names
cyclosporin Arapamycin
02

Targets

mTOR (Mammalian target of rapamycin kinase)CN (Calcineurin)GR (Glucocorticoid receptor)

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