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Once Daily Tacrolimus
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the transcription of pro-inflammatory cytokines.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the transcription of pro-inflammatory cytokines. Used for Organ transplant rejection prophylaxis (kidney, heart, liver), Atopic dermatitis, Autoimmune conditions (off-label use).
At a glance
| Generic name | Once Daily Tacrolimus |
|---|---|
| Also known as | Advagraf® |
| Sponsor | University of Saskatchewan |
| 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 inhibits calcineurin phosphatase, preventing dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells). This blocks the production of IL-2 and other cytokines essential for T-cell proliferation and immune response. The once-daily formulation represents an extended-release version designed to improve dosing convenience and potentially reduce peak-trough fluctuations compared to immediate-release tacrolimus.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver)
- Atopic dermatitis
- Autoimmune conditions (off-label use)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache)
- Hypertension
- Hyperglycemia
- Infection
- Gastrointestinal disturbances
Key clinical trials
- Allogeneic Hematopoietic Stem Cell Transplant for GATA2 Mutations (PHASE2)
- Neurocognitive Function Changes With Extended-Release Tacrolimus Among Older Kidney Transplant Recipients (PHASE4)
- Evaluation of the Benefits of Administering Immunosuppressive Drugs as Single Daily Doses Over the First Year After Liver Transplantation (EASY) (PHASE4)
- Allogeneic Hematopoietic Cell Transplantation for Disorders of T-cell Proliferation and/or Dysregulation (PHASE2)
- A Study to Examine the Efficacy and Safety of Zanubrutinib Given to Adults With Primary Membranous Nephropathy (PHASE2, PHASE3)
- Motor Neurone Disease - Systematic Multi-Arm Adaptive Randomised Trial (PHASE2, PHASE3)
- Valganciclovir Prophylaxis Versus Preemptive Therapy for Cytomegalovirus in Living Donor Kidney Transplant Recipients (PHASE4)
- Reduced Intensity, Partially HLA Mismatched BMT to Treat Hematologic Malignancies (PHASE1, 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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Once Daily Tacrolimus CI brief — competitive landscape report
- Once Daily Tacrolimus updates RSS · CI watch RSS
- University of Saskatchewan portfolio CI