Envarsus XR (Veloxis Pharmaceuticals)

Envarsus XR (LCP-tacrolimus) is a once-daily, extended-release oral formulation of the immunosuppressant tacrolimus, a calcineurin inhibitor. Developed using proprietary MeltDose drug-delivery technology, it is designed to enhance bioavailability and provide a flatter pharmacokinetic profile with significantly lower peak-to-trough fluctuations compared to immediate-release tacrolimus formulations. It is primarily indicated for the prophylaxis of organ rejection in kidney transplant patients, particularly those converting from twice-daily immediate-release tacrolimus. The drug works by binding to the intracellular protein FKBP12; the resulting complex inhibits calcineurin, a calcium-dependent phosphatase. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby blocking T-cell activation and the production of pro-inflammatory cytokines like interleukin-2.

Brand names

EnvarsusEnvarsus XR

Other names

tacrolimus extended-releaseMeltDose tacrolimus