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Prograf (Tacrolimus)
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress the immune system.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress the immune system. Used for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients, Atopic dermatitis (topical formulation), Autoimmune conditions including rheumatoid arthritis and lupus nephritis.
At a glance
| Generic name | Prograf (Tacrolimus) |
|---|---|
| Also known as | Tacrolimus/Prograf®/FK506, FK506, tacrolimus |
| Sponsor | East Carolina University |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (via FKBP12 binding) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus binds to the immunophilin FKBP12, and this complex inhibits calcineurin, a key phosphatase required for dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells). This prevents T-cell receptor signaling and IL-2 production, thereby suppressing T-cell mediated immune responses. It is more potent than cyclosporine and is widely used in transplantation and autoimmune conditions.
Approved indications
- Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients
- Atopic dermatitis (topical formulation)
- Autoimmune conditions including rheumatoid arthritis and lupus nephritis
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia
- Neurotoxicity (tremor, headache)
- Infections
- Hyperkalemia
- Gastrointestinal disturbances
Key clinical trials
- Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia (PHASE2)
- Radiation- and Alkylator-free Bone Marrow Transplantation Regimen for Patients With Dyskeratosis Congenita (PHASE2)
- Tocilizumab in Lung Transplantation (PHASE2)
- Use of Belatacept to Delay Tacrolimus Initiation in Kidney Transplant Patients With Delayed Graft Function
- A Study to Investigate the Efficacy and Safety of Frexalimab Versus Tacrolimus in Adults Undergoing Kidney Transplantation (PHASE2, PHASE3)
- Campath/Fludarabine/Melphalan Transplant Conditioning for Non-Malignant Diseases (PHASE1, PHASE2)
- MT2025-35 Allogeneic Hematopoietic Stem Cell Transplantation Using Reduced Intensity Conditioning Treosulfan and Fludarabine, With Post-Transplant Cytoxan (PTCy) for the Treatment of Hematological Diseases (PHASE2)
- Impact of Envarsus XR® on Kidney Biopsy Subclinical Rejection and Blood Immunologic Profile (PHASE2, PHASE3)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |