LSI-301

LSI-301 is an intravenous reformulation of the small molecule calcineurin inhibitor tacrolimus, developed by LipoSeuticals. Tacrolimus exerts its immunosuppressive effect by binding to the intracellular protein FK506-binding protein 12 (FKBP12), forming a complex that inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and subsequent nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby blocking the transcription of interleukin-2 and other cytokines essential for T-lymphocyte activation. LSI-301 is being developed for use in organ transplantation and oncology, potentially utilizing LipoSeuticals' proprietary lipid-based delivery technology to improve the safety or efficacy profile of the standard intravenous formulation (Prograf).

Other names

tacrolimusPrograf