Fexaramine

[2] When administered orally to mice, fexaramine produced selective actions through FXR receptors in the intestines.

[3] Consistent with the effects of other FXR agonist drugs,[4] in a study in mice, oral fexaramine stimulated intestinal fibroblast growth factor 15 (FGF15) production and resulted in metabolic improvements.

Intestinal tissue-specific actions of fexaramine were suggested to be a possible new approach for the treatment of obesity and metabolic syndrome.

[3] However it cannot be determined from these preliminary results in mice whether FXR agonism with fexaramine will produce weight loss in humans.

There are no clinical trials of fexaramine planned in humans and therapy with such FXR agonists for obesity is only a theoretical approach.

Crystallographic structure of the ligand binding domain of the farnesoid X receptor (rainbow colored cartoon, N-terminus = blue, C-terminus = red) complexed with fexaramine depicted as spheres (carbon = white, oxygen = red, nitrogen = blue). [ 2 ]