Yosprala Wins FDA Nod for Secondary Prevention of Cardio- and Cerebrovascular Events in Patients at Risk for Aspirin-Induced Gastric Ulcers

Fixed-dose combo consists of enteric-coated aspirin core surrounded by omeprazole

The FDA has approved once-daily Yosprala (Aralez Pharmaceuticals), a fixed-dose combination of enteric-coated aspirin, an antiplatelet agent, and omeprazole, a proton pump inhibitor (PPI). Yosprala is indicated for patients who require aspirin for secondary prevention of cardiovascular (CV) and cerebrovascular events and who are at risk of developing aspirin-associated gastric ulcers. The U.S. promotional launch of Yosprala is expected to begin in the first week of October.

Yosprala was designed to support both cardio- and gastro-protection for at-risk patients through the proprietary Intelli-COAT system, which is formulated to sequentially deliver immediate-release omeprazole (40 mg) followed by a delayed-release, enteric-coated aspirin core in either 81-mg or 325-mg strengths. The immediate-release omeprazole in Yosprala is designed to elevate the gastric pH into a gastroprotective zone. The enteric-coated aspirin dissolves after the pH has been elevated to 5.5 or greater, thereby reducing the risk of stomach ulcers.

The FDA’s approval of Yosprala was based on results from two randomized, double-blind, controlled studies in which subjects were randomly assigned to receive either Yosprala 325 mg/40 mg (n = 524) or 325 mg of enteric-coated aspirin (n = 525). Both studies achieved their primary endpoints, with patients in the Yosprala arms experiencing significantly fewer endoscopically confirmed gastric ulcers compared with those receiving enteric-coated aspirin (325 mg) alone.

In addition, significantly fewer patients treated with Yosprala discontinued therapy because of prespecified upper gastrointestinal (GI) adverse events compared with patients in the enteric-coated aspirin arm. The most common adverse events associated with Yosprala included gastritis, nausea, diarrhea, gastric polyps, and noncardiac chest pain.

The aspirin component of Yosprala is indicated for reducing the combined risk of death and nonfatal stroke in patients who have experienced ischemic stroke or transient ischemia of the brain due to fibrin platelet emboli; for reducing the combined risk of death and nonfatal myocardial infarction (MI) in patients with a previous MI or unstable angina pectoris; and for reducing the combined risk of MI and sudden death in patients with chronic stable angina pectoris. It is also indicated for use in patients who have undergone revascularization procedures––coronary artery bypass graft or percutaneous transluminal coronary angioplasty––when there is a pre-existing condition for which aspirin is already indicated.

The omeprazole component of Yosprala is indicated for reducing the risk of developing aspirin-associated gastric ulcers due to age (55 years or greater) or a documented history of gastric ulcers.

Yosprala is not for use as the initial dose of aspirin therapy during the onset of an acute coronary syndrome or acute MI, or before percutaneous coronary intervention. Yosprala was evaluated in clinical studies for the reduction of gastric ulcers. It was not evaluated for the reduction of GI bleeding and therefore has not been shown to reduce the risk of GI bleeding due to aspirin. Yosprala is not interchangeable with the individual components of aspirin and omeprazole.

Source: Aralez Pharmaceuticals; September 15, 2016.