Last reviewed 2026-05-24 · How we verify

Tacrolimus sustained-release capsule

Tacrolimus sustained-release capsule is a Calcineurin inhibitor Small molecule drug developed by Astellas Pharma China, Inc.. It is currently FDA-approved for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients, Atopic dermatitis (eczema), Autoimmune conditions requiring immunosuppression. Also known as: FK506.

Tacrolimus inhibits calcineurin phosphatase, suppressing T-cell activation and proliferation to prevent organ rejection and treat autoimmune conditions.

Tacrolimus sustained-release capsule is used to treat conditions such as renal transplant rejection, liver transplant rejection, and nephrotic syndrome. It works by inhibiting calcineurin, a protein involved in the activation of T-lymphocytes, according to its mechanism of action as recorded in ChEMBL.

At a glance

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 blocks the transcription of IL-2 and other cytokines essential for T-cell proliferation and immune response. The sustained-release formulation provides prolonged drug exposure with potentially improved tolerability and more stable immunosuppression compared to immediate-release formulations.

Approved indications

• Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients
• Atopic dermatitis (eczema)
• Autoimmune conditions requiring immunosuppression

Common side effects

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

Key clinical trials

• Prospective, Multicenter Clinical Study of Prolonged-release Tacrolimus in Stable Pediatric Liver Transplant Recipients (NA)
• Efficacy and Safety Study of the Switch From Cyclosporin to Tacrolimus in Renal Transplant Recipients (PHASE4)
• Early Conversion of Prolonged-release Tacrolimus in Liver Transplantation. (PHASE4)
• Efficacy and Safety of Tacrolimus Sustained-release Capsules in Induction Phase Treatment in Lupus Nephritis (PHASE3)
• Efficacy and Safety of Tacrolimus Sustained-release Capsules in Induction Treatment in Refractory Lupus Nephritis (PHASE3)
• The Efficacy and Tolerance of Tacrolimus Sustained-release Capsules on Refractory Nephrotic Syndrome (RNS) (PHASE3)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Tacrolimus sustained-release capsule CI brief — competitive landscape report
• Tacrolimus sustained-release capsule updates RSS · CI watch RSS
• Astellas Pharma China, Inc. portfolio CI

Frequently asked questions about Tacrolimus sustained-release capsule

Related

• Drug class: All Calcineurin inhibitor drugs
• Target: All drugs targeting Calcineurin (via FKBP12 binding)
• Manufacturer: Astellas Pharma China, Inc. — full pipeline
• Therapeutic area: All drugs in Immunology
• Indication: Drugs for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients
• Indication: Drugs for Atopic dermatitis (eczema)
• Indication: Drugs for Autoimmune conditions requiring immunosuppression
• Also known as: FK506

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing