saka, Japan, February 28, 2014 --- Takeda Pharmaceutical Company Limited (“Takeda”) announced today that it has submitted a New Drug Application to the Ministry of Health, Labour and Welfare for TAK-438 (generic name: Vonoprazan Fumarate). TAK-438, which was discovered by Takeda, is an acid secretion inhibitor belonging to a new class of inhibitors called potassium-competitive acid blockers (P-CABs) that demonstrate strong and sustainable acid secretion inhibitory effects and show efficacy in early termination by competitively inhibiting the binding of potassium ion (K⁺) to H⁺, K⁺-ATPase (proton pump) in the final step of gastric acid secretion in gastric parietal cells.

Takeda has conducted Phase III clinical trials for TAK-438 in Japan for indications including erosive esophagitis, gastric ulcer, duodenal ulcer, and H. pylori eradication. TAK-438 demonstrated efficacy and has a favorable profile for safety and tolerability. The application was based on favorable results obtained from these trials.

Proton pump inhibitors (PPIs) are currently widely prescribed as first-line therapy for the treatment of acid-related diseases in Japan. However, PPIs do not always provide sufficient therapeutic efficacy, and the acid secretion inhibitory effects of PPIs may differ among individuals, because of the protein CYP2C19, which has gene polymorphisms that are involved in metabolism. TAK-438 inhibits proton pumps without the need for activation by acid, and the compound is distributed at high concentrations into the stomach, the target organ, thereby exerting a nearly maximum inhibitory effect from the first dose and remaining effective for 24 hours. Unlike PPIs, TAK-438 is not primarily metabolized by CYP2C19 (which has gene polymorphisms). Since TAK-438 is stable in acid and its immediate-release formulation is available without requiring an optimized formulation design (e.g., enteric-coating), the onset of efficacy does not significantly differ among treated patients. With these advantages, TAK-438 is expected to be a new therapeutic agent that resolves issues with current treatments for acid-related diseases.

"We are extremely pleased to submit the new drug application for TAK-438, which would represent a new treatment option for patients with acid-related diseases that require inhibition of acid secretion," said Nancy Joseph-Ridge M.D., General Manager of Takeda's Pharmaceutical Development Division. "Takeda aims to achieve better treatment outcomes in the field of gastrointestinal diseases and will work hard to meet the medical needs of more patients."