Drug intelligence / Profile preview

cyclosporine + sirolimus

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

Overview

Cyclosporine + sirolimus is a combination of two immunosuppressive drugs commonly used together in organ transplantation, particularly kidney transplantation, to prevent allograft rejection. Cyclosporine is a calcineurin inhibitor that inhibits T-cell activation by blocking interleukin-2 production. Sirolimus (also known as rapamycin) is an mTOR (mammalian target of rapamycin) inhibitor that prevents T-cell proliferation by inhibiting the cellular response to interleukin-2. These drugs work synergistically to suppress the immune response more effectively than either alone, but their combination increases the risk of nephrotoxicity and metabolic side effects. The combination requires careful therapeutic drug monitoring due to significant pharmacokinetic interactions and additive toxicities[4][5][6][7][8].

Other names
cyclosporin A + sirolimusCsA + SRLcyclosporine + rapamycin
02

Targets

ABCB1 (P-glycoprotein)CN (Calcineurin)ABCG2 (Breast cancer resistance protein)CYP3A4 (Cytochrome P450 3A4)mTOR (Mammalian target of rapamycin kinase)

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