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tacrolimus + methylprednisolone
- Development stage
- Unknown
- Lead developer
- Astellas Pharma
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous, Intramuscular
01
Overview
Tacrolimus + methylprednisolone is a combination of two immunosuppressive agents frequently used in clinical practice for the prevention and treatment of organ transplant rejection and management of severe inflammatory or autoimmune conditions. Tacrolimus is a calcineurin inhibitor that suppresses T-lymphocyte activation by inhibiting calcineurin phosphatase activity after binding to the immunophilin FKBP-12. Methylprednisolone is a synthetic glucocorticoid that exerts anti-inflammatory and immunosuppressive effects by modulating gene expression through the glucocorticoid receptor. The combination has demonstrated synergistic immunosuppressive effects and allows for steroid dose reduction while maintaining efficacy[2][1]. It has been studied in settings such as allogeneic bone marrow transplantation for graft-versus-host disease prophylaxis[1], solid organ transplantation[6], and severe COVID-19 with hyperinflammatory syndrome[4].
- Brand names
- Prograf + MedrolAdvagraf + MedrolAstagraf + Medrol
- Other names
- FK506 + methylprednisolone
02
Targets
GR (Glucocorticoid receptor)PPP3CA (Protein phosphatase 3 catalytic subunit alpha)
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