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Tacrolimus (TAC)
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation. Used for Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas), Atopic dermatitis, Severe rheumatoid arthritis.
At a glance
| Generic name | Tacrolimus (TAC) |
|---|---|
| Also known as | Prograf®, FK506, TAC, Protopic, Prograf |
| Sponsor | ITB-Med LLC |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus binds to the immunophilin FKBP12, and this complex inhibits calcineurin phosphatase activity. By blocking calcineurin, it prevents dephosphorylation and nuclear translocation of NFAT, a transcription factor required for IL-2 and other cytokine production. This results in potent immunosuppression, making it effective for preventing organ rejection and treating autoimmune conditions.
Approved indications
- Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas)
- Atopic dermatitis
- Severe rheumatoid arthritis
- Autoimmune uveitis
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia
- Neurotoxicity (tremor, headache)
- Infections
- Hyperkalemia
- Gingival hyperplasia
Key clinical trials
- Assessment of Biomarker-Guided CNI Substitution In Kidney Transplantation (PHASE2)
- Study of Efficacy, Safety, Tolerability, Pharmacokinetic (PK) and Pharmacodynamic (PD) of an Anti-CD40 Monoclonal Antibody, CFZ533, in Kidney Transplant Recipients (PHASE2)
- A Dose Escalation Study of TCD601 Compared to ATG in de Novo Renal Transplantation (PHASE2)
- A Phase I/II GVHD Prevention Trial Combining Pacritinib With Sirolimus-Based Immune Suppression (PHASE1, PHASE2)
- EVR and EPO for Liver Transplant Tolerance (PHASE1)
- Utilization of a Microdevice for Psoriasis and Atopic Dermatitis (PHASE4)
- HMCT/CT2401: Abatacept GVHD Prophylaxis Following Omidubicel HCT (EARLY_PHASE1)
- A Study of TCD601 in de Novo Renal Transplant Recipients (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:
- Tacrolimus (TAC) CI brief — competitive landscape report
- Tacrolimus (TAC) updates RSS · CI watch RSS
- ITB-Med LLC portfolio CI