Drug intelligence / Profile preview

tacrolimus + leflunomide

Development stage
Unknown
Lead developer
King Chulalongkorn Memorial Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

Tacrolimus + leflunomide is a combination therapy being evaluated for the treatment of BK virus (BKV) infection in kidney transplant recipients. Tacrolimus is a calcineurin inhibitor that serves as a cornerstone of post-transplant immunosuppression by preventing T-lymphocyte activation. Leflunomide is an immunomodulatory agent that inhibits dihydroorotate dehydrogenase (DHODH), an enzyme essential for de novo pyrimidine synthesis. In addition to its immunosuppressive properties, leflunomide has demonstrated antiviral activity against the BK polyomavirus, likely by interfering with viral DNA replication or virion assembly. This specific combination, often involving a reduction in the tacrolimus dose to lower the overall immunosuppressive burden, is being studied by King Chulalongkorn Memorial Hospital as a strategy to clear BKV viremia and prevent BKV-associated nephropathy (BKVAN) while maintaining graft protection.

Other names
FK-506 + leflunomidetacrolimus + leflunomide-King Chulalongkorn Memorial Hospital-BK virus infection
02

Targets

FKBP1AFKBP (FK506-binding protein family)CN (Calcineurin)DHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)Tyrosine kinase

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