Review article: the opportunities and benefits of extended acid suppression

Abstract

SUMMARYAcid suppression therapy with proton pump inhibitors is associated with well-established benefits in the management of gastro-oesophageal reflux (GERD) and other acid-related disorders. However, a number of issues still remain unsettled. Despite their clinical efficacy, when given once daily, currently available proton pump inhibitors may not adequately control intragastric acidity during the night in a significant proportion of both healthy subjects and GERD patients, in whom symptom relief remains suboptimal.Although some novel proton pump inhibitors have been synthesized, only few reached clinical testing. Amongst them, tenatoprazole represents a true advance displaying a long half-life (five to seven times longer than that of currently available drugs) and extended acid suppression covering both day and night. All the available clinical studies suggest both pharmacokinetic and pharmacodynamic advantages of tenatoprazole over esomeprazole. As this last compound providesamongst the members of the class -the most effective control of intragastric pH whatever the parameter considered, it is conceivable that tenatoprazole could similarly be better than the other existing proton pump inhibitors.Tenatoprazole appears to be a promising proton pump inhibitor for the treatment of acid-related diseases, where it has the potential to address unmet clinical needs.

Proton pump inhibitors in gastroesophageal reflux disease: a custom-tailored therapeutic regimen

“…A randomized clinical trial (CT) reported that esomeprazole 80 mg was more effective than lansoprazole 60 mg in maintaining intragastric pH > 4 for > 16 h; the split dose of omeprazole was more effective than the standard dose in maintaining pH control (29). No differences in daytime pH control were observed with different omeprazole dosing regimens (40-0-0, 0-0-40 mg versus 20-0-20 mg) during 7 days (n = 18 healthy subjects); the split dose was superior in controlling nighttime intragastric pH than the standard dose given in the morning or in the night (60 vs. 30 vs. 20%; p = 0,02) (28).…”

E3710, Long-Acting PPI as New Approach for the Treatment of Unmet Medical Needs for GERD

“…The potent and long-acting PPI would be feasible for the treatment of gastrointestinal bleeding [Katz et al, 2006;Scarpignato and Pelosini, 2006]. The success rate of Helicobacter pylori eradication therapy depends on intragastric pH, so a long-acting PPI would be acceptable [Katz et al, 2006;Scarpignato and Pelosini, 2006]. Optimizing the control of intragastric pH would also be beneficial in these ARDs, so that a potent and long-acting PPI such as E3710 would be expected to offer improved clinical outcomes for patients with these ARDs as well as GERD.…”

“…The current PPIs are not able to maintain intragastric pH>6 for prolonged periods. The potent and long-acting PPI would be feasible for the treatment of gastrointestinal bleeding [Katz et al, 2006;Scarpignato and Pelosini, 2006]. The success rate of Helicobacter pylori eradication therapy depends on intragastric pH, so a long-acting PPI would be acceptable [Katz et al, 2006;Scarpignato and Pelosini, 2006].…”

“…The widespread use of NSAID and aspirin would involve the risk of drug-related ulcers especially for the patients including personal history of complicated ulcer diseases, concurrent use of NSAID or aspirin, use of high doses, concurrent use of anticoagulant, personal history of uncomplicated peptic ulcer disease, age>70 and concurrent use of steroid. For these patients, concomitant use of promising PPIs with NSAID and/or aspirin would be useful to protect ulcers [Katz et al, 2006;Scarpignato and Pelosini, 2006]. E3710 possesses the appropriate stability in the point view of physical and chemical characteristics, combinational formulation of E3710 with NSAID and/or aspirin therefore may be expected.…”

Proton Pump Inhibitors in Veterinary Medicine

“…The pharmacological acid suppression in these diseases, especially in ulcers and GERD, causes very important benefits, such as abolition of elective surgery and reduction in non-steroidal anti-inflammatory drugs-associated gastropaties (Scarpignato and Pelosini, 2006).…”