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Tacrolimus (Arm B)
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing nuclear translocation of NFAT transcription factors.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing nuclear translocation of NFAT transcription factors. Used for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | Tacrolimus (Arm B) |
|---|---|
| Also known as | Prograf |
| Sponsor | Weill Medical College of Cornell University |
| 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. This prevents NFAT from entering the nucleus and activating genes required for T-cell cytokine production and proliferation. The result is potent immunosuppression, making it effective for preventing organ rejection and treating autoimmune conditions.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas)
- Atopic dermatitis
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache, paresthesia)
- Hypertension
- Hyperglycemia
- Infection
- Hyperkalemia
- Gastrointestinal disturbances
Key clinical trials
- Allogeneic Hematopoietic Stem Cell Transplant for GATA2 Mutations (PHASE2)
- Enhanced Dermatological Care to Reduce Rash and Paronychia in Epidermal Growth Factor Receptor (EGRF)-Mutated Non-Small Cell Lung Cancer (NSCLC) Treated First-line With Amivantamab Plus Lazertinib (PHASE2)
- Graft Versus Host Disease-Reduction Strategies for Donor Blood Stem Cell Transplant Patients With Acute Leukemia or Myelodysplastic Syndrome (MDS) (PHASE2)
- Allo HSCT for High Risk Hemoglobinopathies (PHASE2)
- Treatment of Antibody-Mediated Rejection (ABMR) With CarBel (PHASE2)
- Trial of Cell Based Therapy for DMD (PHASE1)
- A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome (PHASE2)
- Axatilimab Plus Standard of Care Therapy for the Prevention of Graft Versus Host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation in Patients With Hematologic Cancer, ABRAXAS Trial (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 |