tacrolimus + methotrexate

Tacrolimus + methotrexate is a combination of two immunosuppressive drugs used primarily in the management of autoimmune diseases such as rheumatoid arthritis, particularly in patients who have an insufficient response to methotrexate alone. Tacrolimus is a calcineurin inhibitor that suppresses T-cell activation by binding to FKBP12 and inhibiting calcineurin phosphatase activity, thereby reducing IL-2 transcription and other cytokines involved in T-cell activation[8]. Methotrexate is an antimetabolite that inhibits enzymes responsible for nucleotide synthesis, including dihydrofolate reductase, leading to suppression of cell division and anti-inflammatory effects[6]. The combination has been shown to reduce relapse risk after TNF inhibitor discontinuation and improve disease control compared to monotherapy with either agent[1][2][4][5]. Both drugs are associated with potential nephrotoxicity when used together[3].

Other names

FK506 (for tacrolimus)MTX (for methotrexate)