{"id":"tacrolimus-prolonged-release-formulation","safety":{"commonSideEffects":[{"rate":null,"effect":"Nephrotoxicity / renal impairment"},{"rate":null,"effect":"Hypertension"},{"rate":null,"effect":"Hyperglycemia / new-onset diabetes"},{"rate":null,"effect":"Tremor"},{"rate":null,"effect":"Headache"},{"rate":null,"effect":"Infections"},{"rate":null,"effect":"Hyperkalemia"}]},"_chembl":{"chemblId":"CHEMBL3989887","moleculeType":"Small molecule","molecularWeight":"822.05"},"_dailymed":null,"mechanism":{"_ai_source":"claude-haiku-4.5","explanation":"Tacrolimus binds to the immunophilin FKBP12 and forms a complex that inhibits calcineurin phosphatase activity. This prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), blocking the transcription of pro-inflammatory cytokines such as IL-2, IL-4, and TNF-α. The prolonged-release formulation provides sustained drug exposure with potentially improved tolerability and reduced dosing frequency compared to immediate-release formulations.","oneSentence":"Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing immune rejection.","_ai_confidence":"high"},"_scrapedAt":"2026-03-28T00:10:52.122Z","_scrapedBy":"cloudflare-swarm","_wikipedia":null,"indications":{"approved":[{"name":"Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients"},{"name":"Autoimmune diseases including atopic dermatitis and other inflammatory conditions"}]},"trialDetails":[{"nctId":"NCT03644485","phase":"PHASE4","title":"Clinical Outcome of Delayed or Standard Prograf Together With Induction Therapy Followed by Conversion to Advagraf in Donation After Cardiac (or Circulatory) Death (DCD) Kidney Transplant Recipients","status":"COMPLETED","sponsor":"Astellas Pharma China, Inc.","startDate":"2018-10-21","conditions":"Kidney Transplant","enrollment":284},{"nctId":"NCT03216447","phase":"PHASE4","title":"A Study of Patient Adherence and Convenience to Immunosuppressive Agents in Newly Liver Transplant","status":"UNKNOWN","sponsor":"Chang Gung Memorial Hospital","startDate":"2017-11-23","conditions":"Liver Transplantation","enrollment":150},{"nctId":"NCT02432833","phase":"PHASE4","title":"Multicentre, Open Label, Randomized, Two-arm, Parallel-group Study to Assess Efficacy and Safety of ENVARSUS® Compared With Tacrolimus Used as Per Current Clinical Practice in the Initial Maintenance Setting in de Novo Kidney Transplant Patients","status":"COMPLETED","sponsor":"Chiesi Farmaceutici S.p.A.","startDate":"2015-05","conditions":"End Stage Renal Disease","enrollment":428},{"nctId":"NCT02311010","phase":"PHASE4","title":"Practical Use of Advagraf de Novo After Kidney Transplantation According to Recipient Genetic Polymorphism","status":"UNKNOWN","sponsor":"Université Catholique de Louvain","startDate":"2011-01","conditions":"Kidney Diseases","enrollment":150}],"_emaApprovals":[],"_faersSignals":[],"_approvalHistory":[],"publicationCount":33,"rwe":[],"genericFilers":[],"relatedDrugs":[],"labelChanges":[],"biosimilarFilings":[],"pricing":[],"formularyStatus":[],"manufacturing":[],"companionDiagnostics":[],"competitors":[],"timeline":[],"patents":[],"ownershipHistory":[],"trials":[],"biosimilars":[],"latestUpdates":[],"references":[],"tags":[],"ecosystem":[],"genericManufacturerList":[],"offLabel":[],"developmentCodes":[],"aliases":["Advagraf","FK506"],"phase":"marketed","status":"active","brandName":"Tacrolimus prolonged-release formulation","genericName":"Tacrolimus prolonged-release formulation","companyName":"Astellas Pharma China, Inc.","companyId":"astellas-pharma-china-inc","modality":"Small molecule","firstApprovalDate":"","aiSummary":"Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing immune rejection. Used for Prophylaxis of organ rejection in allogeneic kidney, heart, and liver transplant recipients, Autoimmune diseases including atopic dermatitis and other inflammatory conditions.","enrichmentLevel":3,"visitCount":0,"trialStats":{"total":1,"withResults":0},"verificationStatus":"verified","dataCompleteness":{"mechanism":true,"indications":true,"safety":true,"trials":true,"score":4}}