Drug intelligence / Profile preview

tacrolimus + sirolimus + corticosteroids

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous (corticosteroids Only), Subcutaneous (occasionally For Corticosteroids; Very Rare For Others)
01

Overview

This drug is a **combination immunosuppressive regimen** composed of tacrolimus, sirolimus, and corticosteroids. It is utilized primarily to prevent or treat transplant rejection and graft-versus-host disease (GVHD), particularly in settings like kidney transplantation and hematopoietic stem cell transplantation. - **Tacrolimus** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting interleukin-2 (IL-2) production. - **Sirolimus** (rapamycin) inhibits mTOR (mechanistic target of rapamycin), blocking IL-2 driven T-cell and B-cell proliferation independently of calcineurin. - **Corticosteroids** broadly modulate inflammation and immune responses via genomic and non-genomic mechanisms, including suppression of multiple cytokines and leukocyte migration. Together, this combination provides **synergistic immunosuppression** acting at different points in the immune activation cascade, reducing the risk of acute and chronic rejection but with increased risk of adverse effects including renal dysfunction, myelosuppression, infection, hyperlipidemia, and metabolic complications[2][5][6][7]. This regimen is commonly used in patients with steroid-resistant chronic GVHD, kidney and stem cell transplantation, and other situations requiring intense immunosuppression[2][5][6].

Brand names
Prograf + Rapamune + corticosteroids
Other names
FK506 + rapamycin + glucocorticosteroids
02

Targets

CYP3A (CYP3A family)FKBP1AABCB1 (P-glycoprotein)GR (Glucocorticoid receptor)mTOR (Mammalian target of rapamycin kinase)CN (Calcineurin)

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