Envarsus XR Launched for Kidney Transplant Rejection Prophylaxis

Veloxis announced that Envarsus XR (tacrolimus extended-release) tablets are now available for the prophylaxis of rejection in kidney transplant patients converted from immediate-release tacrolimus formulations, in combination with other immunosuppressants.

Envarsus XR is intended for once-daily dosing, providing flatter pharmacokinetics and higher bioavailability compared to twice-daily tacrolimus.

Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin inhibited. Tacrolimus inhibits the expression and/or production of several cytokines, inhibits IL-2 receptor expression and nitric oxide release, induces apoptosis and production of transforming growth factor-beta that can lead to immunosuppressive activity. The net result is the inhibition 13 of T-lymphocyte activation and proliferation as well as T-helper-cell-dependent B-cell response.

Envarsus XR was granted Orphan Drug status by the Food and Drug Administration. It is supplied as 0.75mg, 1mg, and 4mg strength tablets in 30- and 100-count bottles.

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