{"id":"fk506e","safety":{"commonSideEffects":[{"rate":null,"effect":"Nephrotoxicity"},{"rate":null,"effect":"Neurotoxicity (tremor, headache)"},{"rate":null,"effect":"Hypertension"},{"rate":null,"effect":"Hyperglycemia"},{"rate":null,"effect":"Infections"},{"rate":null,"effect":"Gum hyperplasia"}]},"_chembl":null,"_dailymed":null,"mechanism":{"_ai_source":"claude-haiku-4.5","explanation":"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.","oneSentence":"FK506E is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, preventing IL-2 production and T-cell proliferation.","_ai_confidence":"medium"},"_scrapedAt":"2026-03-28T01:12:44.150Z","_scrapedBy":"cloudflare-swarm","_wikipedia":null,"indications":{"approved":[{"name":"Prevention of organ rejection in transplant recipients"},{"name":"Autoimmune and inflammatory conditions (phase 3 development)"}]},"trialDetails":[{"nctId":"NCT01294020","phase":"PHASE2","title":"Study to Compare the Pharmacokinetics of Tacrolimus in Stable Pediatric Allograft Recipients Converted From Prograf® to Advagraf®","status":"COMPLETED","sponsor":"Astellas Pharma Europe Ltd.","startDate":"2011-05-25","conditions":"Intestine Transplantation, Kidney Transplantation, Lung Transplantation","enrollment":81},{"nctId":"NCT02723591","phase":"PHASE4","title":"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","status":"COMPLETED","sponsor":"Astellas Pharma Global Development, Inc.","startDate":"2016-09-09","conditions":"Kidney Transplantation","enrollment":599},{"nctId":"NCT02118896","phase":"PHASE3","title":"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","status":"COMPLETED","sponsor":"Astellas Pharma Europe Ltd.","startDate":"2003-02-24","conditions":"Heart Transplantation, Liver Transplantation, Kidney Transplantation","enrollment":850},{"nctId":"NCT01011205","phase":"PHASE3","title":"Phase 3b Study to Evaluate Advagraf in Combination With Mycophenolate Mofetil and Basiliximab in Liver Transplantation","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2009-09-30","conditions":"Liver Transplantation","enrollment":893},{"nctId":"NCT00933231","phase":"PHASE3","title":"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","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2009-08-17","conditions":"Kidney Transplantation","enrollment":281},{"nctId":"NCT01304836","phase":"PHASE4","title":"A Study Looking at Diabetes in Kidney Transplant Recipients Receiving Immunosuppressive Regimen With or Without Steroids","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2011-01-22","conditions":"Kidney Transplantation","enrollment":1166},{"nctId":"NCT02555787","phase":"","title":"Global, Multicentre, Non Interventional Advagraf Conversion Registry in Kidney Transplant Patients","status":"COMPLETED","sponsor":"Astellas Pharma Europe Ltd.","startDate":"2015-03-05","conditions":"Kidney Transplantation","enrollment":4430},{"nctId":"NCT01363752","phase":"PHASE4","title":"A Study Looking at Kidney Function in Kidney Transplant Recipients Who Are Taking Anti-rejection Medication Including Tacrolimus and With or Without Sirolimus.","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2011-03-08","conditions":"Kidney Transplantation","enrollment":853},{"nctId":"NCT01339468","phase":"PHASE4","title":"A Study to Assess the Pharmacokinetics, Safety and Efficacy of Advagraf and Prograf in de Novo Liver Transplantation","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2011-04-27","conditions":"Liver Transplantation","enrollment":100},{"nctId":"NCT01018914","phase":"PHASE4","title":"A Study to Compare Safety and Efficacy of Prograf + Myfortic and Advagraf + Myfortic in Liver Transplantation Patients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2009-04","conditions":"Liver Transplantation","enrollment":44},{"nctId":"NCT01332201","phase":"PHASE2","title":"Study to Compare the Pharmacokinetics of Tacrolimus in Adult Transplant Recipients Treated With Advagraf® or Prograf®","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2011-07","conditions":"Heart Transplantation, Lung Transplantation, Pancreas (Including SPK) Transplantation","enrollment":17},{"nctId":"NCT02377609","phase":"","title":"To Validate an Analytical Method to Measure Concentration of Tacrolimus in Blood Taken From Finger Pricks","status":"TERMINATED","sponsor":"Astellas Pharma Europe Ltd.","startDate":"2013-10","conditions":"Validation, Dried Blood Spot, Transplant Patients","enrollment":108},{"nctId":"NCT01435291","phase":"PHASE4","title":"AADAPT - Analysis of Advagraf Dose Adaptation Post Transplantation","status":"COMPLETED","sponsor":"Centre Hospitalier Universitaire de Nice","startDate":"2011-10","conditions":"Renal Transplantation","enrollment":45},{"nctId":"NCT00865137","phase":"PHASE3","title":"An Open Study Assessing Bioavailability of a Modified Formulation of Tacrolimus in Kidney Transplant Recipients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2007-09","conditions":"Kidney Transplantation","enrollment":27},{"nctId":"NCT00481481","phase":"PHASE3","title":"Conversion Study From Cyclosporine to FK506MR Based Immunosuppression in Kidney Transplant Subjects","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2007-04","conditions":"Transplantation","enrollment":346},{"nctId":"NCT00384202","phase":"PHASE3","title":"A Conversion Study to Assess Safety and Efficacy of a MR4 Based Immunosuppressive Regimen in Stable Liver Recipients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2006-10","conditions":"Transplantation","enrollment":112},{"nctId":"NCT00189839","phase":"PHASE3","title":"A Study to Evaluate the Safety and Efficacy of FK506E (MR4) in Patients Undergoing Primary Kidney Transplantation","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2004-08","conditions":"Kidney Transplantation","enrollment":699},{"nctId":"NCT00818194","phase":"PHASE1","title":"Comparison of Extended Release Tacrolimus (Advagraf) and Cyclosporine A Microemulsion on Renal Function in Healthy Volunteers","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2008-04","conditions":"Healthy","enrollment":18},{"nctId":"NCT00189826","phase":"PHASE3","title":"A Study to Evaluate the Safety and Efficacy of FK506E (MR4) in Patients Undergoing Primary Liver Transplantation.","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2004-08","conditions":"Liver Transplantation","enrollment":475},{"nctId":"NCT00384137","phase":"PHASE3","title":"A Conversion Study to Assess Safety and Efficacy of a MR4 Based Immunosuppressive Regimen in Stable Kidney Recipients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2006-10","conditions":"Transplantation","enrollment":128},{"nctId":"NCT00282256","phase":"PHASE2","title":"A Study of a Modified-Release Tacrolimus Based Immunosuppression Regimen in Stable Pediatric Liver Transplant Patients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2004-01","conditions":"Liver Transplantation","enrollment":19},{"nctId":"NCT00282243","phase":"PHASE2","title":"A Study to Assess the Pharmacokinetics of a Modified-release Tacrolimus Based Immunosuppression Regimen in Stable Liver Transplant Patients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2003-02","conditions":"Liver Transplantation","enrollment":70},{"nctId":"NCT00282568","phase":"PHASE2","title":"A Study to Assess the Pharmacokinetics of a Modified-release Tacrolimus Based Immunosuppression Regimen in Stable Kidney Transplant Patients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2002-08","conditions":"Kidney Transplantation","enrollment":70},{"nctId":"NCT01839929","phase":"PHASE4","title":"A Study to Assess the Safety and Efficacy of ADVAGRAF (Tacrolimus Modified Release Formulation) in Kidney Transplant Patients Who Were Treated With PROGRAF","status":"COMPLETED","sponsor":"Astellas Pharma Korea, Inc.","startDate":"2010-09","conditions":"Kidney Transplantation","enrollment":138},{"nctId":"NCT01681134","phase":"PHASE1","title":"A Comparison of the Effects of Extended Release Tacrolimus (Advagraf®) vs. Immediate Release Tacrolimus (Prograf®) on Kidney Function in Healthy Male Volunteers","status":"COMPLETED","sponsor":"Astellas Pharma Canada, Inc.","startDate":"2012-07","conditions":"Healthy","enrollment":19},{"nctId":"NCT00909571","phase":"PHASE3","title":"Pharmacokinetics of Tacrolimus in Liver Transplantation Patients Treated With Prograf and Modified Release Tacrolimus","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2009-04","conditions":"Liver Transplantation","enrollment":10},{"nctId":"NCT00720408","phase":"PHASE3","title":"A Randomized Study to Assess the Safety and Efficacy of Prograf vs Prograf-XL in de Novo Liver Transplant Recipients.","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2007-12","conditions":"Liver Transplantation, Transplantation Immunology, Host vs Graft Reaction","enrollment":48},{"nctId":"NCT00719745","phase":"PHASE3","title":"A Study to Assess the Safety and Efficacy of Prograf and MR4 in Liver Transplant Recipients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2006-02","conditions":"Liver Transplantation","enrollment":74},{"nctId":"NCT00720265","phase":"PHASE3","title":"A Study to Assess the Safety and Efficacy of Prograf and MR4 in Kidney Transplantation Patients","status":"COMPLETED","sponsor":"Astellas Pharma Inc","startDate":"2006-02","conditions":"Kidney Transplantation","enrollment":135}],"_emaApprovals":[],"_faersSignals":[],"_approvalHistory":[],"publicationCount":0,"rwe":[],"genericFilers":[],"relatedDrugs":[],"labelChanges":[],"biosimilarFilings":[],"pricing":[],"formularyStatus":[],"manufacturing":[],"companionDiagnostics":[],"competitors":[],"timeline":[],"patents":[],"ownershipHistory":[],"trials":[],"biosimilars":[],"latestUpdates":[],"references":[],"tags":[],"ecosystem":[],"genericManufacturerList":[],"offLabel":[],"developmentCodes":[],"aliases":["Astagraf XL","Advagraf","Graceptor","MR4","Prograf XL"],"phase":"phase_3","status":"active","brandName":"FK506E","genericName":"FK506E","companyName":"Astellas Pharma Europe Ltd.","companyId":"astellas-pharma-europe-ltd","modality":"Small molecule","firstApprovalDate":"","aiSummary":"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).","enrichmentLevel":3,"visitCount":1,"trialStats":{"total":1,"withResults":1},"verificationStatus":"verified","dataCompleteness":{"mechanism":true,"indications":true,"safety":true,"trials":true,"score":4}}