Drug intelligence / Profile preview

tacrolimus (modified release) + steroids

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

Overview

**Tacrolimus (modified release) + steroids** is a combination immunosuppressive regimen, typically used in organ transplantation and certain autoimmune nephropathies (like refractory IgA nephropathy), consisting of a prolonged- or extended-release formulation of tacrolimus (a calcineurin inhibitor) together with a steroid (commonly prednisone or methylprednisolone, corticosteroids). - **Tacrolimus (modified release)** acts primarily by binding to the immunophilin FKBP12, forming a complex that inhibits calcineurin, ultimately blocking T-cell activation and interleukin-2 (IL-2) transcription, thus suppressing cellular immune response[2][4][6]. - **Steroids (e.g., prednisone, methylprednisolone)** exert their immunosuppressive and anti-inflammatory effects via binding to the glucocorticoid receptor, altering transcription of various inflammatory and immune target genes. This combination is used to enhance immunosuppressive efficacy and reduce the risk of organ rejection or to induce remission in autoimmune nephropathies[1][5].

Brand names
AdvagrafAstagraf XLEnvarsus XR (for tacrolimus modified release)multiple steroid brand names (prednisone, methylprednisolone, etc.)
Other names
tacrolimus prolonged release + steroidstacrolimus extended release + corticosteroidstacrolimus MR + steroids
02

Targets

GR (Glucocorticoid receptor)

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