NEW YORK (Reuters Health) – A molecular complex of aspirin and phosphatidylcholine called PL2200 seems to protect against acute gastroduodenal erosion and ulceration in older adults at risk for aspirin-related ulcers.

PL2200 is being developed by PLx Pharma of Houston, Texas. It has been shown to have equivalent bioavailability to immediate release aspirin, based on both pharmacokinetic analysis and antiplatelet efficacy.

In a randomized, single-blind, multicenter study, investigators compared upper GI damage in 204 healthy subjects following 7 days of immediate release aspirin (325 milligrams once daily) or one PL2200 capsule also containing 325 mg aspirin.

According to a report published online November 16 in the American Journal of Gastroenterology, participants were between 50 and 74 years old and all underwent a baseline endoscopy to evaluate their GI mucosa and again after 7 days of aspirin or PL2200 treatment.

In the intent-to-treat population (102 in the aspirin arm and 99 in the PL2200 arm), subjects treated with PL2200 had a 47.4% lower risk of developing multiple gastroduodenal erosions or an ulcer than subjects treated with aspirin for 7 days.

Overall, 43 of aspirin-treated subjects (42.2%) developed multiple erosions and/or ulcers, compared with 22 PL2200-treated subjects (22.2%; P = 0.0027). Consistently, the PL2200 group had a lower mean number of gastric erosions than the aspirin group (2.26 vs 3.83; P = 0.0009), the investigators report.

The PL2200 group also had a 71% lower incidence of gastroduodenal ulcers relative to the aspirin group. Day 7 endoscopy showed ulcers in 5 subjects in the PL2200 arm (5.1%) versus 18 in the aspirin arm (17.6%), a statistically significant difference (P = 0.0069).

Similar results were seen in the per-protocol analysis (90 in the aspirin arm and 91 in the PL2200 arm). All ulcers detected by endoscopy were asymptomatic and predominantly in the stomach.

“This study provides proof of concept that this mechanism of non-covalent association of aspirin with phosphatidylcholine is a strategy that effectively reduces gastrointestinal ulceration, at least within the short term,” first author Dr. Byron Cryer, of University of Texas Southwestern and VA North Texas Health Care System, Dallas, noted in an e-mail to Reuters Health.

“This study’s observations are important from a public health perspective since low-dose aspirin is so widely used and gastric ulceration is one of the more concerning adverse effects of aspirin,” he added.

There were no clinically or statistically significant differences in treatment-related adverse events with PL2200 and aspirin. The most frequently reported events were nausea, dyspepsia, and heartburn. These events, which tended to be reported more often in the PL2200 group, usually resolved after the first several days.

Because PL2200 provides GI protection in a way akin to proton pump inhibitors (by minimizing local disruption of the GI barrier), “PL2200 could be an alternative or complement to PPIs as an effective strategy to reduce GI injury in high-risk patients,” Dr. Cryer and colleagues say.

“As a next step, it will be important to follow-up this study’s observations with trials of longer periods of aspirin administration to evaluate whether (PL2200) continues to have a similar ability to reduce aspirin’s gastrointestinal risks with longer periods of observation,” Dr. Cryer told Reuters Health.

The study was conducted with grant support from the National Institute of Diabetes and Digestive and Kidney Diseases and from PLx Pharma.