Drug intelligence / Profile preview

turofexorate isopropyl

Development stage
Discontinued
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

Turofexorate isopropyl is a potent, selective, and orally bioavailable small molecule agonist of the farnesoid X receptor (FXR), also known as the bile acid receptor. It was originally discovered by Exelixis and later licensed to Wyeth, which became a subsidiary of Pfizer. The drug binds to the ligand-binding domain of human FXR and promotes transcription of genes involved in bile acid metabolism such as BSEP, SHP, and IBABP. Turofexorate isopropyl has demonstrated activity in suppressing lipid peroxidation and inhibiting ferroptotic cell death through FXR activation. It was investigated for metabolic diseases including hyperlipidemia, atherosclerosis, and nonalcoholic steatohepatitis (NASH), but development has been discontinued at phase 1[2][3][4][5][6].

Other names
turofexorate isopropyl
02

Targets

FXR (Farnesoid x-activated receptor)

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