Last reviewed · How we verify
Low Tacrolimus
Low-dose tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby reducing immune-mediated rejection and inflammation.
Low-dose tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by blocking the phosphatase calcineurin, thereby reducing immune-mediated rejection and inflammation. Used for Organ transplant rejection prophylaxis (kidney, heart, liver), Autoimmune and inflammatory conditions (off-label use in some settings).
At a glance
| Generic name | Low Tacrolimus |
|---|---|
| Also known as | Low Prograf |
| Sponsor | Ronaldo de Matos Esmeraldo, MD |
| 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 inhibits calcineurin phosphatase activity, preventing dephosphorylation and nuclear translocation of NFAT transcription factors. This blocks IL-2 and other cytokine production critical for T-cell proliferation. Low-dose formulations aim to maintain therapeutic immunosuppression while reducing nephrotoxicity and other dose-dependent adverse effects.
Approved indications
- Organ transplant rejection prophylaxis (kidney, heart, liver)
- Autoimmune and inflammatory conditions (atopic dermatitis, eczema)
Common side effects
- Nephrotoxicity
- Neurotoxicity (tremor, headache)
- Hypertension
- Hyperglycemia
- Infection
- 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:
- Low Tacrolimus CI brief — competitive landscape report
- Low Tacrolimus updates RSS · CI watch RSS
- Ronaldo de Matos Esmeraldo, MD portfolio CI