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Tacrolimus (Prograf®)
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 Prevention of organ rejection in kidney, heart, and liver transplant recipients, Atopic dermatitis (topical formulation), Severe refractory uveitis.
At a glance
| Generic name | Tacrolimus (Prograf®) |
|---|---|
| Also known as | Prograf |
| Sponsor | Astellas Pharma 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 activation and proliferation. This potent immunosuppression makes it effective for preventing organ rejection and treating autoimmune conditions.
Approved indications
- Prevention of organ rejection in kidney, heart, and liver transplant recipients
- Atopic dermatitis (topical formulation)
- Severe refractory uveitis
- Autoimmune conditions (off-label use)
Common side effects
- Nephrotoxicity/renal dysfunction
- Hypertension
- Hyperglycemia/new-onset diabetes
- Neurotoxicity (tremor, headache, paresthesia)
- Infections
- Hyperkalemia
- Gastrointestinal disturbances
Key clinical trials
- Impact of Envarsus XR® on Kidney Biopsy Subclinical Rejection and Blood Immunologic Profile (PHASE2, PHASE3)
- HLA-Mismatched Unrelated Donor Hematopoietic Cell Transplantation With Post-Transplantation Cyclophosphamide (PHASE2)
- High Dose Ruxolitinib and Allogeneic Stem Cell Transplantation in Myelofibrosis Patients With Splenomegaly (PHASE2)
- Treatment of Antibody-Mediated Rejection (ABMR) With CarBel (PHASE2)
- A Blood Stem Cell Transplant for Sickle Cell Disease (PHASE1)
- Tocilizumab in Cardiac Transplantation (PHASE2)
- Advancing Transplantation Outcomes in Children (PHASE2)
- Utilising Genotype Informed Bayesian Dosing of Tacrolimus in Children Post Solid Organ Transplantation. (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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Tacrolimus (Prograf®) CI brief — competitive landscape report
- Tacrolimus (Prograf®) updates RSS · CI watch RSS
- Astellas Pharma Inc portfolio CI