Drug intelligence / Profile preview

prednisolone + tacrolimus

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Prednisolone + tacrolimus is a combination therapy consisting of two immunosuppressive agents. Prednisolone (or its closely related prodrug prednisone) is a synthetic glucocorticoid corticosteroid that suppresses inflammation and modulates immune responses by binding to the glucocorticoid receptor and altering gene transcription. Tacrolimus is a calcineurin inhibitor that prevents T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby reducing interleukin-2 production and other cytokines critical for immune response. This combination is primarily used in conditions requiring potent immunosuppression such as nephrotic syndrome with mesangial proliferation and in organ transplantation to prevent rejection. The combination has demonstrated efficacy in inducing remission in nephrotic syndrome and improving transplant outcomes, though it requires careful monitoring due to potential pharmacokinetic interactions that can increase drug exposure or toxicity[1][3][6].

Other names
prednisone + tacrolimustacrolimus + prednisolonetacrolimus + prednisone
02

Targets

GR (Glucocorticoid receptor)FKBP1ACN (Calcineurin)

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