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Oral Tab Tacrolimus
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing the transcription of pro-inflammatory cytokines.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby preventing the transcription of pro-inflammatory cytokines. Used for Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | Oral Tab Tacrolimus |
|---|---|
| Sponsor | NephroNet, Inc. |
| 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 phosphatase activity. By blocking calcineurin, it prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), which is essential for IL-2 and other cytokine gene transcription. 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
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia
- Tremor
- Headache
- Infection
- Hyperkalemia
- Neurotoxicity (encephalopathy)
Key clinical trials
- Study of Efficacy, Safety, Tolerability, Pharmacokinetic (PK) and Pharmacodynamic (PD) of an Anti-CD40 Monoclonal Antibody, CFZ533, in Kidney Transplant Recipients (PHASE2)
- 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)
- De-escalated Cyclophosphamide (PTCy) and Ruxolitinib for Graft-versus-Host Disease (GVHD) Prophylaxis (PHASE2)
- Motor Neurone Disease - Systematic Multi-Arm Adaptive Randomised Trial (PHASE2, PHASE3)
- BIVV020 (SAR445088) in Prevention and Treatment of Antibody-mediated Rejection (AMR) (PHASE2)
- Pulse Wave Velocity, Tacrolimus Time in Therapeutic Range and CV in African American Kidney Transplants (PHASE4)
- Extended-Release Tacrolimus Following Liver Transplantation (PHASE4)
- Oral Tacrolimus vs Dexamethasone Micro-pulse Therapy in Pediatric Rapidly Progressing Vitiligo: A Multicenter RCT (NA)
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:
- Oral Tab Tacrolimus CI brief — competitive landscape report
- Oral Tab Tacrolimus updates RSS · CI watch RSS
- NephroNet, Inc. portfolio CI