China-based Jiangsu Hengrui Medicine Co., Ltd (SHA: 600276) announced that it has received market approval from the National Medical Products Administration (NMPA) for its generic version of Astellas’s tacrolimus. The drug is approved for use in the prevention of graft rejection after kidney transplantation, prevention of graft rejection in the maintenance period after liver transplantation, and treatment of graft rejection after kidney or liver transplantation that cannot be controlled by other immunosuppressive drugs. This marks the first generic of its type to be approved in China.
Drug Mechanism
At the molecular level, tacrolimus enters the cell and binds to the FKBP12 protein to form a complex. This complex competitively binds and inhibits calcineurin, thereby inhibiting the intracellular-calcium-dependent signal transduction channel in T cells and preventing a series of lymphokine gene transcriptions. In vivo and in vitro experiments have confirmed that tacrolimus is a potent immunosuppressant. It can inhibit the generation of cytotoxic lymphocytes that cause transplant rejection, inhibit the activation of T cells and the proliferation of T helper cell-dependent B cells, and inhibit the production of lymphokines (such as interleukin 2, interleukin 3, and gamma interferon) and the expression of interleukin 2 receptors.
Global Sales and Approval History
Tacrolimus was first approved in Denmark, Latvia, Holland, and the Czech Republic in 2007. It was subsequently approved in Japan and the US under the trade names of Graceptor and Astagraf XL in 2008 and 2013, respectively. The drug generated USD 3.16 billion in global sales in 2021.-Fineline Info & Tech
