Farnesoid X receptor modulators (2011 - 2014): a patent review summarizes recent patents and publications regarding FXR modulators. The farnesoid X receptor regulates bile acid metabolism and its activation has potential therapeutic benefits for cholestatic disorders and fatty liver disease. The review covers new chemical entities that modulate FXR and their efficacy shown in in vitro and in vivo studies from 2011 to 2014, with a focus on their patent status. While FXR agonists have demonstrated therapeutic potential in clinical trials for conditions like primary biliary cirrhosis and fatty liver disease, side effects remain a challenge.

1. Farnesoid X receptor modulators
(2011 - 2014): a patent review.
Expert Opin Ther Pat. 2015 Aug;25(8):885-96
Sepe V, Distrutti E, Fiorucci S, Zampella A.

2. Expert Opin Ther Pat. 2015 Aug;25(8):885-96
• Introduction: Farnesoid-X-receptor (FXR) is the receptor for primary bile
acids expressed in enterohepatic tissues where it regulates bile acid
uptake, metabolism and disposal. For its role as a bile acid sensor, FXR has
been thought to be an important target in the treatment of cholestatic
disorders, a family of diseases in which endogenous bile acids accumulate
in the body. Cholestasis might occur as a consequence of inborn metabolic
errors and three major disorders, intra-hepatic cholestasis in pregnancy,
primary biliary cirrhosis (PBC) and primary sclerosing cholangitis account
for the vast majority of clinical cholestasis occurring in adulthood. In
addition, FXR agonists are gaining attention as potential regulators of lipid
and glucose metabolism and therefore as new therapeutical approaches
to the treatment of fatty liver disease, type 2 diabetes and obesity.
• Areas covered: New chemical entities as FXR modulators and their in vitro
and in vivo efficacy are reviewed with particular focus on patents and
peer-reviewed publications in the period 2011 – 2014.
• Expert opinion: FXR agonists have shown robust therapeutic potential and
results from clinical trials have supported their use in the treatment of
liver disorders including PBC and fatty liver disease despite side effects.