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Maintenance of immediate-release tacrolimus
Maintenance of immediate-release tacrolimus is a Calcineurin inhibitor Small molecule drug developed by Massachusetts General Hospital. It is currently FDA-approved for Maintenance immunosuppression in organ transplant recipients (kidney, heart, liver, pancreas), Prevention of organ rejection in transplant patients. Also known as: Prograf.
Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the transcription of pro-inflammatory cytokines, thereby preventing organ rejection.
Tacrolimus inhibits calcineurin phosphatase, blocking T-cell activation and proliferation to prevent organ rejection. Used for Maintenance immunosuppression in organ transplant recipients (kidney, heart, liver, pancreas), Prevention of organ rejection in transplant patients.
At a glance
| Generic name | Maintenance of immediate-release tacrolimus |
|---|---|
| Also known as | Prograf |
| Sponsor | Massachusetts General 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 inhibits calcineurin phosphatase, which prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells). This blocks the transcription of interleukin-2 and other cytokines essential for T-cell proliferation and differentiation. The immediate-release formulation provides rapid absorption for acute immunosuppression, while maintenance therapy sustains long-term graft tolerance.
Approved indications
- Maintenance immunosuppression in organ transplant recipients (kidney, heart, liver, pancreas)
- Prevention of organ rejection in transplant patients
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia
- Tremor
- Headache
- Infection
- Hyperkalemia
- Neurotoxicity (including PRES)
Key clinical trials
- Neurocognitive Function Changes With Extended-Release Tacrolimus Among Older Kidney Transplant Recipients (PHASE4)
- Tacrolimus Trial for Hereditary Hemorrhagic Telangiectasia (HHT) (PHASE2)
- Comparison of Tacrolimus Extended-Release (Envarsus XR) to Tacrolimus Immediate-Release in Human Leukocyte Antigen (HLA) Sensitized Kidney Transplant Recipients (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:
- Maintenance of immediate-release tacrolimus CI brief — competitive landscape report
- Maintenance of immediate-release tacrolimus updates RSS · CI watch RSS
- Massachusetts General Hospital portfolio CI
Frequently asked questions about Maintenance of immediate-release tacrolimus
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Related
- Drug class: All Calcineurin inhibitor drugs
- Target: All drugs targeting Calcineurin (via FKBP12 binding)
- Manufacturer: Massachusetts General Hospital — full pipeline
- Therapeutic area: All drugs in Immunology
- Indication: Drugs for Maintenance immunosuppression in organ transplant recipients (kidney, heart, liver, pancreas)
- Indication: Drugs for Prevention of organ rejection in transplant patients
- Also known as: Prograf
- Compare: Maintenance of immediate-release tacrolimus vs similar drugs
- Pricing: Maintenance of immediate-release tacrolimus cost, discount & access