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Tacrolimus immediate-release formulation
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress immune responses.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress immune responses. Used for Organ transplant rejection prophylaxis (kidney, heart, liver), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | Tacrolimus immediate-release formulation |
|---|---|
| Also known as | Prograf, FK506 |
| Sponsor | Astellas Pharma China, Inc. |
| 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 essential 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 required for T-cell proliferation and differentiation. This potent immunosuppressive effect makes it valuable in transplantation and autoimmune conditions.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver)
- Atopic dermatitis
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache, paresthesia)
- Hypertension
- Hyperglycemia
- Infections
- Gastrointestinal disturbances
Key clinical trials
- Extended Release Versus Immediate Release Tacrolimus Following Renal Allograft Failure to Reduce Allosensitisation (PHASE4)
- Effect of Tacrolimus Formulation on Neurological Side Effects in Older Kidney Transplant Recipients (PHASE4)
- Clinical Outcome of Delayed or Standard Prograf Together With Induction Therapy Followed by Conversion to Advagraf in Donation After Cardiac (or Circulatory) Death (DCD) Kidney Transplant Recipients (PHASE4)
- Comparison of Tacrolimus Extended-Release (Envarsus XR) to Tacrolimus Immediate-Release in Human Leukocyte Antigen (HLA) Sensitized Kidney Transplant Recipients (PHASE4)
- Envarsus XR in Lung Transplant (PHASE2)
- Envarsus XR® in Adolescent Renal Transplant Recipients (PHASE4)
- Tacrolimus Pharmacokinetic Subpopulations
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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