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FK506E
FK506E is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation.
FK506E 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, Autoimmune and inflammatory conditions (phase 3 development).
At a glance
| Generic name | FK506E |
|---|---|
| Also known as | Astagraf XL, Advagraf, Graceptor, MR4, Prograf XL |
| Sponsor | Astellas Pharma Europe Ltd. |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | Phase 3 |
Mechanism of action
FK506E (tacrolimus extended-release formulation) binds to the immunophilin FKBP12 and inhibits calcineurin phosphatase activity. This prevents dephosphorylation of NFAT transcription factors, blocking their nuclear translocation and subsequent IL-2 and other cytokine gene expression. The result is potent suppression of T-cell mediated immune responses, making it useful for transplant rejection prevention and autoimmune conditions.
Approved indications
- Prevention of organ rejection in transplant recipients
- Autoimmune and inflammatory conditions (phase 3 development)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache)
- Hypertension
- Hyperglycemia
- Infections
- Gum hyperplasia
Key clinical trials
- Study to Compare the Pharmacokinetics of Tacrolimus in Stable Pediatric Allograft Recipients Converted From Prograf® to Advagraf® (PHASE2)
- To Compare the Effects of Immediate-release Tacrolimus and Astagraf XL on Donor-Specific Antibody (DSA) Formation and the Development of Immune Activation (IA) in de Novo Kidney Transplant Recipients (PHASE4)
- Study to Ascertain if Prolonged Release Tacrolimus (FK506E - MR4) is Safe and Effective When Used in the Long Term and in Combination With Other Immunosuppressive Drugs in Patients Who Have Received a Transplant (PHASE3)
- Phase 3b Study to Evaluate Advagraf in Combination With Mycophenolate Mofetil and Basiliximab in Liver Transplantation (PHASE3)
- Comparison of Standard Versus Low Dose Advagraf® With or Without Angiotensin-converting Enzyme Inhibitor (ACEi)/Angiotensin Receptor Blocker (ARB) on Histology and Function of Renal Allografts (PHASE3)
- A Study Looking at Diabetes in Kidney Transplant Recipients Receiving Immunosuppressive Regimen With or Without Steroids (PHASE4)
- Global, Multicentre, Non Interventional Advagraf Conversion Registry in Kidney Transplant Patients
- A Study Looking at Kidney Function in Kidney Transplant Recipients Who Are Taking Anti-rejection Medication Including Tacrolimus and With or Without Sirolimus. (PHASE4)
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:
- FK506E CI brief — competitive landscape report
- FK506E updates RSS · CI watch RSS
- Astellas Pharma Europe Ltd. portfolio CI