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LCP-tacrolimus
LCP-tacrolimus is a lipid-conjugated prodrug of tacrolimus that inhibits calcineurin to suppress T-cell activation and proliferation.
LCP-tacrolimus is a lipid-conjugated prodrug of tacrolimus that inhibits calcineurin to suppress T-cell activation and proliferation. Used for Organ transplant rejection prevention, Graft-versus-host disease (GVHD).
At a glance
| Generic name | LCP-tacrolimus |
|---|---|
| Also known as | Envarsus® |
| Sponsor | University Hospital Tuebingen |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Tacrolimus is a calcineurin inhibitor that prevents dephosphorylation of NFAT, blocking IL-2 and other cytokine production critical for T-cell activation. The lipid conjugation (LCP formulation) enhances lymphoid tissue targeting and oral bioavailability, allowing improved immunosuppression with potentially reduced systemic exposure compared to conventional tacrolimus.
Approved indications
- Organ transplant rejection prevention
- Graft-versus-host disease (GVHD)
Common side effects
- Nephrotoxicity
- Neurotoxicity
- Hyperglycemia
- Hypertension
- Infections
Key clinical trials
- Evaluation of the Benefits of Administering Immunosuppressive Drugs as Single Daily Doses Over the First Year After Liver Transplantation (EASY) (PHASE4)
- Tacrolimus and Risk Factors for Glucose Metabolism Disorders in Kidney Transplant Patients
- Evaluation of Anti-rejection Drug, Tacrolimus, in African-Americans With Kidney Transplant (PHASE4)
- Early Use of Long-acting Tacrolimus in Lung Transplant Recipients (EARLY_PHASE1)
- P-glypoprotein Inhibition Effect on the Pharmacokinetics of Two Tacrolimus Formulations: Prolonged and Extended-release (PHASE2)
- Tacrolimus Formulation and Glucose Metabolism After Kidney Transplantation (TAGLUMET Trial) (PHASE4)
- Tacrolimus Associated Tremors in Liver Transplantation: Immediate-Release Versus Extended-Release Formulations (PHASE4)
- PK Study in Diabetic Transplant récipients : From Twice-daily Tacrolimus to Once-daily Extended-release Tacrolimus (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 |