Drug intelligence / Profile preview

dexamethasone + 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, Topical
01

Overview

Dexamethasone + tacrolimus is a compounded combination of two immunosuppressive agents used primarily for their synergistic anti-inflammatory and immunomodulatory effects. Dexamethasone is a synthetic corticosteroid that suppresses inflammation and modulates immune responses by binding to the glucocorticoid receptor, thereby inhibiting pro-inflammatory gene expression. Tacrolimus is a calcineurin inhibitor that prevents T-cell activation by inhibiting calcineurin phosphatase activity, leading to reduced interleukin-2 (IL-2) transcription and T-cell proliferation. This combination has been used in various formulations (such as oral liquid or topical solutions) for conditions like chronic graft-versus-host disease (cGVHD), autoimmune hepatitis, inflammatory bowel disease, dermatological conditions, organ transplantation management, and immune thrombocytopenia[1][5][9]. The combined use may require careful monitoring due to pharmacokinetic interactions; corticosteroids like dexamethasone can induce CYP3A enzymes and P-glycoprotein activity, potentially lowering blood levels of tacrolimus[2][3].

02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)

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