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tacrolimus, low dose
tacrolimus, low dose is a Calcineurin inhibitor Small molecule drug developed by Hoffmann-La Roche. It is currently FDA-approved for Organ transplant rejection prophylaxis (kidney, heart, liver), Atopic dermatitis, Atopic keratoconjunctivitis.
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 small molecule inhibitor of the peptidyl-prolyl cis-trans isomerase FKBP1A, classified as an INHIBITOR. It is used to treat conditions such as end-stage renal failure with renal transplant, kidney transplant, and traumatic wounds and injuries, among others, often in combination with other immunosuppressive agents.
At a glance
| Generic name | tacrolimus, low dose |
|---|---|
| Sponsor | Hoffmann-La Roche |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| 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. This prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), blocking the production of IL-2, IFN-γ, and other cytokines essential for T-cell proliferation and immune response. Low-dose formulations are used to minimize systemic immunosuppression while maintaining therapeutic benefit in specific indications.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver)
- Atopic dermatitis
- Atopic keratoconjunctivitis
- Vernal keratoconjunctivitis
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache, paresthesia)
- Hypertension
- Hyperglycemia
- Hyperkalemia
- Infection (due to immunosuppression)
- Gingival hyperplasia
Key clinical trials
- Reduced Intensity Haploidentical BMT for High Risk Solid Tumors (PHASE2)
- A Study to Examine the Efficacy and Safety of Zanubrutinib Given to Adults With Primary Membranous Nephropathy (PHASE2, PHASE3)
- A Phase II Study of Allogeneic Hematopoietic Stem Cell Transplant for Subjects With VEXAS (Vacuoles, E1 Enzyme, X-linked, Autoinflammatory, Somatic) Syndrome (PHASE2)
- REgulatory T Cell Therapy to Achieve Immunosuppression REduction (PHASE2)
- Efficacy + Safety of Liposome Cyclosporine A to Treat Bronchiolitis Obliterans Post Double Lung Transplant (BOSTON-2) (PHASE3)
- A Study of the Safety and Tolerability of ASP7317 in Senior Adults Who Are Losing Their Clear, Sharp Central Vision Due to Geographic Atrophy Secondary to Dry Age-related Macular Degeneration (PHASE1)
- Dose-Expansion Study of Low Dose Post-Transplant Cyclophosphamide/Tacrolimus/Ruxolitinib for Graft-versus-Host Disease (GVHD) Prophylaxis in Myeloablative Allogeneic Peripheral Blood Stem Cell Transplantation (PHASE2)
- VEL-101 to Prevent Rejection After Kidney Transplantation (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, low dose CI brief — competitive landscape report
- tacrolimus, low dose updates RSS · CI watch RSS
- Hoffmann-La Roche portfolio CI
Frequently asked questions about tacrolimus, low dose
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Related
- Drug class: All Calcineurin inhibitor drugs
- Target: All drugs targeting Calcineurin (protein phosphatase 2B)
- Manufacturer: Hoffmann-La Roche — full pipeline
- Therapeutic area: All drugs in Immunology
- Indication: Drugs for Organ transplant rejection prophylaxis (kidney, heart, liver)
- Indication: Drugs for Atopic dermatitis
- Indication: Drugs for Atopic keratoconjunctivitis
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing