GW4064 is a potent, orally-available, non-steroidal, isoxazole-based agonist of FXR with an EC50 of 15 nM. In a Fisher rat model, GW4064 was found to lower serum triglyceride levels in a dose-dependent manner and an ED50 of 20 mg/kg. (1)

In C57BL/6 mice, GW4064 has been shown to stimulate plasma corticosterone levels, thus suggesting a role in the modulation of adrenal cholesterol metabolism and glucocorticoid synthesis. (2)

Followup SAR studies have led to equipotent FXR analogs of GW4064 with improved developability parameters, including reduced toxicity and cholestasis. (3)

GW4064 is a potent, orally-available, non-steroidal, isoxazole-based agonist of FXR with an EC50 of 15 nM. In a Fisher rat model, GW4064 was found to lower serum triglyceride levels in a dose-dependent manner and an ED50 of 20 mg/kg. (1)

In C57BL/6 mice, GW4064 has been shown to stimulate plasma corticosterone levels, thus suggesting a role in the modulation of adrenal cholesterol metabolism and glucocorticoid synthesis. (2)

Followup SAR studies have led to equipotent FXR analogs of GW4064 with improved developability parameters, including reduced toxicity and cholestasis. (3)