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Tacrolimus - Prograf® twice daily formulation
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress the immune response.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress the immune response. Used for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | Tacrolimus - Prograf® twice daily formulation |
|---|---|
| Also known as | Prograf® |
| Sponsor | University of British Columbia |
| 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 serine/threonine phosphatase critical for dephosphorylating NFAT (nuclear factor of activated T cells). By preventing NFAT translocation to the nucleus, tacrolimus blocks the transcription of IL-2 and other cytokines essential for T-cell proliferation and immune activation. This potent immunosuppressive effect makes it valuable in transplantation and autoimmune conditions.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas)
- Atopic dermatitis
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia/new-onset diabetes
- Neurotoxicity (tremor, headache)
- Infection
- Hyperkalemia
- Gum hyperplasia
Key clinical trials
- Efficacy + Safety of Liposome Cyclosporine A to Treat Bronchiolitis Obliterans Post Double Lung Transplant (BOSTON-2) (PHASE3)
- Efficacy + Safety of Liposome Cyclosporine A to Treat Bronchiolitis Obliterans Post Single Lung Transplant (BOSTON-1) (PHASE3)
- Real-word Study of the de NOVO Extended-release tacrolimuS in Kidney Transplantation Using an ARTificial Intelligence
- Tacrolimus Formulation and Glucose Metabolism After Kidney Transplantation (TAGLUMET Trial) (PHASE4)
- Envarsus XR® in Adolescent Renal Transplant Recipients (PHASE4)
- Efficacy and Safety of a 0.1% Tacrolimus Nasal Ointment as a Treatment for Epistaxis in Hemorrhagic Hereditary Telangiectasia (HHT) (PHASE2)
- Conversion Pharmacodynamic Study in Stable Renal Transplant Patients Receiving Tacrolimus Two Times a Day to a New Formulation of Tacrolimus - LCP Tacro - 1 Time a Day. (PHASE4)
- Comparison of Medication Adherence Between Once and Twice Daily Tacrolimus in Stable Renal Transplant Recipients (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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