Last reviewed 2026-04-22 · How we verify

Tacrolimus, Mylan

Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing the dephosphorylation of nuclear factor of activated T cells (NFAT).

Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing the dephosphorylation of nuclear factor of activated T cells (NFAT). Used for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients, Atopic dermatitis (topical formulation), Autoimmune conditions including rheumatoid arthritis and lupus nephritis.

At a glance

Mechanism of action

Tacrolimus binds to the immunophilin FKBP12, and this complex inhibits calcineurin, a serine/threonine phosphatase essential for T-cell receptor signaling. By preventing NFAT dephosphorylation and nuclear translocation, tacrolimus suppresses the transcription of cytokines (IL-2, TNF-α, IFN-γ) required for T-cell proliferation and differentiation. This potent immunosuppression makes it effective for preventing organ rejection and treating autoimmune conditions.

Approved indications

• Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients
• Atopic dermatitis (topical formulation)
• Autoimmune conditions including rheumatoid arthritis and lupus nephritis

Common side effects

• Nephrotoxicity
• Hypertension
• Hyperglycemia/new-onset diabetes
• Neurotoxicity (tremor, headache)
• Infection
• Hyperkalemia
• Gastrointestinal disturbances

Key clinical trials

• Conversion From Brand to Generic Tacrolimus in High Risk Transplant Recipients (PHASE4)

Primary sources

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