Our Pipeline

Fexuprazan

Fexuprazan is a potassium-competitive acid blocker (P-CAB) that we are initially developing for the treatment of erosive esophagitis (EE).

 

  • EE is a severe form of gastroesophageal reflux disease (GERD) caused by the inflammation, irritation and swelling of the lining of the esophagus, resulting in sores or erosions of the esophageal lining and, in some cases, GI bleeding. EE is classified by erosions in the gastric mucosa caused by acidic reflux of stomach contents into the esophagus.

 

  • The current standard of care for the treatment of EE are medicines called proton pump inhibitors (PPIs).

 

  • Fexuprazan is a member of an emerging class of therapeutics known as P-CABs, which have been shown to improve GI acid blocking activity relative to PPIs. P-CABs bind reversibly to the potassium binding site of the hydrogen potassium ATPase enzyme, or proton pump, to inhibit its activity, thus preventing acid production. Unlike PPIs, as illustrated in the figure below, P-CABs do not require activation by gastric acid and bind with slow dissociation rates to both active and inactive proton pumps. They also have a longer plasma half-life than PPIs.

 

  • In Phase 2 and Phase 3 clinical trials conducted by Daewoong Pharmaceutical Co., Ltd., (Daewoong) in South Korea, Fexuprazan demonstrated efficacy in healing erosions in patients with EE. Fexuprazan has been approved for the treatment of EE in South Korea.

 

  • We have exclusively licensed the U.S. and Canadian rights to Fexuprazan from Daewoong.

NG101

NG101 is an oral, small molecule peripherally acting dopamine D2 receptor antagonist currently in Phase 2 clinical development for the treatment of gastroparesis.

 

  • Gastroparesis is a chronic, severe and debilitating disorder that may be associated with dysfunction in the enteric nervous system, causing the movement of food from the stomach to the small intestine to slow or stop, and preventing or disrupting normal digestion. Patients with gastroparesis often limit their intake of food and liquids, leading to poor nutrition and dehydration, which in turn can ultimately require hospitalization.

 

D2 receptor antagonists are an established class of therapeutics with demonstrated efficacy in relieving gastroparesis symptoms; however, their use has been limited because they are associated with an increased risk of serious CNS and cardiac side effects.

 

  • NG101 is a proprietary mesylate salt form of metopimazine, a D2 receptor antagonist that has not been associated with an increased risk of serious CNS or cardiac side effects. Metopimazine has been approved and prescribed in France for over 40 years for the symptomatic treatment of nausea and vomiting and has been shown to be safe and generally well-tolerated for those indications. Metopimazine has never been evaluated for the treatment of gastroparesis.

 

We are conducting a 12-week, randomized, double-blind, placebo-controlled Phase 2 clinical trial of NG101, in which we are enrolling patients with moderate to severe idiopathic or diabetic gastroparesis.

 

We hold the worldwide rights to NG101.

 

Learn about our clinical trial