-2%
Tacrograf, a calcineurin inhibitor, is an immunosuppressant used for the prophylaxis of organ rejection in both adult and pediatric patients undergoing:
- Liver transplant
- Kidney transplant
- Heart transplant
- Lung transplant
It is used in combination with other immunosuppressants, such as corticosteroids, azathioprine, or mycophenolate mofetil (MMF).
Tacrograf contains tacrolimus, which binds to the intracellular protein FKBP-12. This binding forms a complex with calcium, calmodulin, and calcineurin, thereby inhibiting calcineurin’s phosphatase activity.
Key pharmacological effects:
- Cytokine inhibition: Reduces the expression and/or production of cytokines, including:
- IL-1β, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8, IL-10
- γ-Interferon
- Tumor necrosis factor-alpha (TNF-α)
- Immune suppression:
- Inhibits activation and proliferation of T-lymphocytes.
- Suppresses T-helper cell-dependent B-cell responses.
- Reduces nitric oxide release and induces apoptosis.
Outcome: Prevents immune-mediated rejection of transplanted organs