Astagraf XL (tacrolimus extended-release capsules; Astellas) has been approved for the prophylaxis of organ rejection in patients receiving a kidney transplant with mycophenolate mofetil (MMF) and corticosteroids, with or without basiliximab induction. Astagraf XL is the first once-daily oral tacrolimus formulation available in the U.S. for kidney transplant patients.
The approval was based on two primary, randomized, comparative Phase 3 clinical studies that included 1,093 patients (545 on tacrolimus extended-release) in the U.S., Europe, Canada, South America, Australia and South Africa.
Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action is not known. Experimental evidence suggests that 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.
This effect may prevent the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines (such as interleukin-2, gamma interferon). The net result is the inhibition of T-lymphocyte activation (i.e., immunosuppression).
For more information call (800) 727-7003 or visit US.Astellas.com.