for the treatment of gastroparesis
Gastroparesis is a syndrome characterized by delayed gastric emptying in the absence of mechanical obstruction of the stomach. The etiology of gastroparesis may be diverse, but most cases are classified as idiopathic or occurring secondary to diabetes mellitus. Population-based studies have shown that approximately 20% of patients with diabetes have upper GI symptoms. There is currently no adequate treatment for nausea and vomiting associated with gastroparesis and hospitalization is often required for moderate-to-severe cases. The only approved therapy in the US, metoclopramide (Reglan), has significant CNS toxicities resulting in a black box warning limiting use to 12-weeks. Domperidone is another dopamine antagonist approved in Europe and was available through a compassionate use IND in the US. However, in July 2013 the FDA banned this use due to cardiovascular toxicity issues. Pure pro-kinetic approaches (attempts to increase gastric motility) have not been successful so far, indicating that nausea and vomiting are important symptoms of gastroparesis not alleviated by pro-kinetic action alone.
NG101 is a potent, selective and peripherally restricted dopamine D2/D3 receptor antagonist. NG101 is a safe, well tolerated and highly effective antiemetic compound that has been approved and prescribed in Europe for decades for the treatment of acute conditions. NG101 does not cross the blood-brain-barrier and therefore is not associated with central side effects. In addition, NG101 is not associated with cardiovascular side effects.
Neurogastrx is developing NG101 for the treatment of gastroparesis. We have generated preclinical data indicating that in addition to its potent antiemetic properties, NG101 is also expected to significantly increase gastric motility, conferring NG101 an ideal pharmacological profile for the treatment of gastroparesis.