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Tacrolimus - Advagraf® once daily 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 Prophylaxis of organ rejection in adult patients receiving allogeneic kidney, heart, or liver transplants, Rejection prophylaxis in pediatric transplant recipients.
At a glance
| Generic name | Tacrolimus - Advagraf® once daily formulation |
|---|---|
| Also known as | Advagraf® |
| 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 key phosphatase required for dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells). This prevents transcription of IL-2 and other cytokines essential for T-cell proliferation. Advagraf® is a once-daily extended-release formulation designed to improve patient adherence compared to twice-daily immediate-release tacrolimus.
Approved indications
- Prophylaxis of organ rejection in adult patients receiving allogeneic kidney, heart, or liver transplants
- Rejection prophylaxis in pediatric transplant recipients
Common side effects
- Tremor
- Headache
- Hypertension
- Nephrotoxicity/elevated creatinine
- Hyperglycemia/new-onset diabetes
- Infections
- Hyperkalemia
- Nausea
Key clinical trials
- Comparison of Medication Adherence Between Once and Twice Daily Tacrolimus in Stable Renal Transplant Recipients (PHASE4)
- Multicentre, Open Label, Randomized, Two-arm, Parallel-group Study to Assess Efficacy and Safety of ENVARSUS® Compared With Tacrolimus Used as Per Current Clinical Practice in the Initial Maintenance Setting in de Novo Kidney Transplant Patients (PHASE4)
- Evaluation Of Switching From Twice Daily Tacrolimus To Once Daily Formulation On Cardiovascular Risk (PHASE4)
- Insulin Secretion and Advagraf (PHASE4)
- A Study to Assess the Pharmacokinetics of a Modified-release Tacrolimus Based Immunosuppression Regimen in Stable Liver Transplant Patients (PHASE2)
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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