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immediate-release tacrolimus
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress immune responses.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to suppress immune responses. Used for Organ transplant rejection prophylaxis (kidney, heart, liver), Atopic dermatitis, Autoimmune conditions (off-label use in various settings).
At a glance
| Generic name | immediate-release tacrolimus |
|---|---|
| Also known as | Prograf |
| Sponsor | University of Minnesota |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (serine/threonine phosphatase) |
| 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 critical for dephosphorylating NFAT (nuclear factor of activated T cells). By preventing NFAT translocation to the nucleus, tacrolimus blocks the transcription of IL-2 and other cytokines essential for T-cell proliferation and differentiation. The immediate-release formulation provides faster absorption compared to extended-release formulations.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver)
- Atopic dermatitis
- Autoimmune conditions (off-label use in various settings)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache, paresthesia)
- Hypertension
- Hyperglycemia
- Infection
- Gastrointestinal disturbances
- Hyperkalemia
Key clinical trials
- Neurocognitive Function Changes With Extended-Release Tacrolimus Among Older Kidney Transplant Recipients (PHASE4)
- VEL-101 to Prevent Rejection After Kidney Transplantation (PHASE2)
- Envarsus XR Compared to Immediate Release Tacrolimus (PHASE4)
- PK Assessment of Tacrolimus Exposure Before and After a Switch From Twice Daily Immediate-release (Prograf®) to Once-daily Prolonged Release Tacrolimus (Envarsus®) (PHASE4)
- Simplified IMmunosuppressive Protocol Utilizing Low Dose EnvarsusXR (PHASE4)
- Pulse Wave Velocity, Tacrolimus Time in Therapeutic Range and CV in African American Kidney Transplants (PHASE4)
- CIRTEN-Simultaneous Pancreas-Kidney Transplant Recipients (PHASE2, PHASE3)
- Extended Release Versus Immediate Release Tacrolimus Following Renal Allograft Failure to Reduce Allosensitisation (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:
- immediate-release tacrolimus CI brief — competitive landscape report
- immediate-release tacrolimus updates RSS · CI watch RSS
- University of Minnesota portfolio CI