Bile acid is a substance synthesized from cholesterol in the liver. After being synthesized in the liver, it is stored in the gallbladder as the main component of bile and secreted from the gallbladder via the bile duct into the duodenum in association with meals. It is involved in digestion and absorption of dietary fat.

Approximately 95% of the secreted bile acids are reabsorbed in the small intestine by enterohepatic circulation, return to the liver via the portal vein, and are again secreted into bile.¹ On the other hand, bile acids that were not reabsorbed reach the large intestine.

It is known that when bile acids increase in the large intestinal lumen, fluid is secreted into the large intestinal lumen by the action of bile acids and gastrointestinal motility is enhanced.^2,3

GOOFICE^® Tablet 5 mg (generic name: elobixibat hydrate) is an oral therapeutic agent for chronic constipation* containing elobixibat as the active ingredient that has an inhibitory effect on bile acid transporters. GOOFICE^® Tablet 5 mg is a low-molecular compound structurally developed based on a compound found in the search for antihyperlipidemic drugs. Elobixibat specifically inhibits the ileal bile acid transporter (IBAT), a transporter involved in reabsorption of bile acids in the terminal ileum.⁴ If reabsorption of bile acids is inhibited by the action of elobixibat on IBAT and the amount of bile acids that reach the large intestine increases, fluid secretion into the large intestinal lumen and gastrointestinal motility are considered to be enhanced. Based on these observations, it is assumed that elobixibat may exert a therapeutic effect on constipation via an unprecedented mechanism of action, and Ajinomoto Pharmaceuticals Co., Ltd. (current EA Pharma Co., Ltd.) started development of the drug as a therapeutic agent for chronic constipation in April 2012.

In Japan, the phase 1 study was started in April 2013, the late phase 2 study in July 2014, and the phase 3 study and the long-term administration study in October to November 2015. The efficacy and safety were evaluated through the joint development with Mochida Pharmaceutical Co., Ltd. As a result, GOOFICE^® Tablet 5 mg was approved for marketing in January 2018 as a therapeutic drug for chronic constipation.*

*: Excluding constipation due to organic disease