Tacrolimus Lipid Suspension for Enema

Tacrolimus Lipid Suspension for Enema is a localized rectal formulation of the calcineurin inhibitor tacrolimus, developed by Jina Pharmaceuticals for the treatment of mild to moderately active left-sided or distal ulcerative colitis. By delivering the drug directly to the site of colonic inflammation via a lipid-based suspension, the formulation aims to achieve high local therapeutic concentrations while reducing the systemic absorption and toxicity typically associated with oral or intravenous tacrolimus. The mechanism involves the inhibition of calcineurin-mediated dephosphorylation of the nuclear factor of activated T-cells (NFAT), which suppresses the transcription of interleukin-2 (IL-2) and other pro-inflammatory cytokines, leading to reduced T-lymphocyte activation and proliferation.

Other names

Tacrolimus enemaTacrolimus rectal suspensionTacrolimus lipid suspension