Last reviewed · How we verify
Branded Tacrolimus
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation. Used for Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas), Atopic dermatitis, Severe rheumatoid arthritis.
At a glance
| Generic name | Branded Tacrolimus |
|---|---|
| Also known as | Prograf |
| Sponsor | Novartis |
| 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 phosphatase activity. By blocking calcineurin, it prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), thereby suppressing the transcription of IL-2 and other pro-inflammatory cytokines essential for T-cell activation and proliferation. This potent immunosuppression makes it effective in preventing organ rejection and treating autoimmune conditions.
Approved indications
- Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas)
- Atopic dermatitis
- Severe rheumatoid arthritis
- Autoimmune uveitis
Common side effects
- Nephrotoxicity/renal impairment
- Hypertension
- Hyperglycemia/new-onset diabetes
- Neurotoxicity (tremor, headache, paresthesia)
- Infection
- Hyperkalemia
- Gastrointestinal disturbances
Key clinical trials
- Study to Compare Pharmacokinetics of Tacrolimus Prolonged-release (PR) Capsules and Advagraf® PR Capsules in Stable Kidney Transplant Patients. (PHASE1)
- Pharmacokinetics of Generic to Brand Tacrolimus in Stable Renal Transplant Patients (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:
- Branded Tacrolimus CI brief — competitive landscape report
- Branded Tacrolimus updates RSS · CI watch RSS
- Novartis portfolio CI