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Tacrolimus capsule
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing transcription of IL-2 and other cytokine genes.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing transcription of IL-2 and other cytokine genes. Used for Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | Tacrolimus capsule |
|---|---|
| Also known as | Tac-arm, Envarsus®XR., tacrobell tablet, Protopic®, Advagraf |
| Sponsor | Oslo University Hospital |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (via FKBP12 binding) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus binds to the immunophilin FKBP12, and this complex inhibits calcineurin, a serine/threonine phosphatase essential for dephosphorylating NFAT (nuclear factor of activated T cells). By preventing NFAT nuclear translocation, tacrolimus suppresses the transcription of interleukin-2 and other T-cell activation genes, resulting in potent immunosuppression. This mechanism makes it effective for preventing organ rejection and treating autoimmune conditions.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver, pancreas)
- Atopic dermatitis
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity/renal impairment
- Hypertension
- Hyperglycemia/new-onset diabetes
- Neurotoxicity (tremor, headache, paresthesia)
- Infections
- Hyperkalemia
- Gastrointestinal disturbances
Key clinical trials
- A Study to Investigate the Efficacy and Safety of Frexalimab Versus Tacrolimus in Adults Undergoing Kidney Transplantation (PHASE2, PHASE3)
- Enhanced Dermatological Care to Reduce Rash and Paronychia in Epidermal Growth Factor Receptor (EGRF)-Mutated Non-Small Cell Lung Cancer (NSCLC) Treated First-line With Amivantamab Plus Lazertinib (PHASE2)
- Graft Versus Host Disease-Reduction Strategies for Donor Blood Stem Cell Transplant Patients With Acute Leukemia or Myelodysplastic Syndrome (MDS) (PHASE2)
- A Study to Evaluate Efficacy, Safety, and Tolerability of Povetacicept in Participants With Primary Membranous Nephropathy (pMN) (PHASE2, PHASE3)
- A Study to Examine the Efficacy and Safety of Zanubrutinib Given to Adults With Primary Membranous Nephropathy (PHASE2, PHASE3)
- Motor Neurone Disease - Systematic Multi-Arm Adaptive Randomised Trial (PHASE2, PHASE3)
- Rectal Indomethacin and Oral Tacrolimus Versus Combination to Prevent Post-ERCP Pancreatitis (PHASE3)
- Study to Compare the Pharmacokinetics of Tacrolimus in Stable Pediatric Allograft Recipients Converted From Prograf® to Advagraf® (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 capsule CI brief — competitive landscape report
- Tacrolimus capsule updates RSS · CI watch RSS
- Oslo University Hospital portfolio CI