Most Read Articles
22 hours ago
There appears to be a high rate of emergency department (ED) admission for acute exacerbation of chronic obstructive pulmonary disease (AECOPD), with patients having significant in-hospital mortality, according to data from the *AANZDEM study. Furthermore, compliance with evidence-based treatments in the ED is suboptimal.
Tristan Manalac, 5 days ago
Of the newly identified genetic loci for primary angle-closure glaucoma (PACG), two are significantly associated with primary angle-closure suspect (PACS), indicating involvement in the earlier stages of the disease, a recent Singapore study has shown.
2 days ago
Resistance training appears to confer significant benefits for inflammation and insulin pathway profiles in postmenopausal breast cancer survivors, according to a study. However, the magnitude and degree of benefit from exercise may be influenced by whether or not women gained strength and/or lost weight during exercise.
Pearl Toh, 2 days ago
Patients with inflammatory bowel disease (IBD) who had primary nonresponse to an anti-tumour necrosis factor (TNF) agent ─ or inadequate response to the initial loading doses ─ were less likely to respond to second-line biologics compared with those who had secondary loss of response (LOR) or intolerance to the primary therapy, according to a systematic review and meta-analysis presented at the Crohn's & Colitis Congress (CCC) 2018 held recently in Las Vegas, Nevada, US.

ONO-8539 a novel therapeutic option for managing heartburn

12 Oct 2017

The novel prostanoid EP1 receptor antagonist ONO-8539 appears to attenuate acid-induced heartburn in healthy men, suggesting that EP1 receptors play a role in generating heartburn symptoms, according to a study.

A total of 20 males were randomized to receive either ONO-8539 (450 mg) or placebo, administered once 4 hours prior to acid perfusion test, during which hydrochloric acid at 0.15 mol l−1 was perfused into the lower oesophagus for half an hour.

Acid perception threshold was calculated as the time to first sensation of heartburn. Severity of upper gastrointestinal (GI) symptoms was assessed using a validated categorical rating scale. Upper GI symptoms of interest included heartburn, sour or bitter taste, pricking pain in the stomach, dull pain in the stomach, heavy feeling in the stomach, tight feeling in the stomach, nausea, and sensation of fullness.

Results revealed that compared with placebo, ONO-8539 significantly reduced total heartburn symptom score, but not other upper GI symptom scores, during acid perfusion (area under the curve, 56.5 with ONO-8539 vs 85.0 with placebo; p<0.01).

Furthermore, the time to first sensation of heartburn was significantly prolonged with ONO-8539 vs placebo (9.7 vs 4.3 minutes; p<0.05).

The present data show ONO-8539 as a potential novel therapeutic option for controlling heartburn symptoms in patients with gastro-oesophageal reflux disease.

ONO-8539 inhibits the EP1 receptor, which is one of the prostaglandin E2 (PGE2) receptors. In particular, oesophageal PGE2 plays an essential role in the induction and generation of heartburn symptoms in humans. Such mechanism of action of ONO-8539 has been classified as ‘‘insurmountable’’ and ‘‘competitive,’’ characterized by a long duration of inhibitory effect due to slow dissociation from the receptors. [Am J Physiol Gastrointest Liver Physiol 2013;304:G568–73]

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Most Read Articles
22 hours ago
There appears to be a high rate of emergency department (ED) admission for acute exacerbation of chronic obstructive pulmonary disease (AECOPD), with patients having significant in-hospital mortality, according to data from the *AANZDEM study. Furthermore, compliance with evidence-based treatments in the ED is suboptimal.
Tristan Manalac, 5 days ago
Of the newly identified genetic loci for primary angle-closure glaucoma (PACG), two are significantly associated with primary angle-closure suspect (PACS), indicating involvement in the earlier stages of the disease, a recent Singapore study has shown.
2 days ago
Resistance training appears to confer significant benefits for inflammation and insulin pathway profiles in postmenopausal breast cancer survivors, according to a study. However, the magnitude and degree of benefit from exercise may be influenced by whether or not women gained strength and/or lost weight during exercise.
Pearl Toh, 2 days ago
Patients with inflammatory bowel disease (IBD) who had primary nonresponse to an anti-tumour necrosis factor (TNF) agent ─ or inadequate response to the initial loading doses ─ were less likely to respond to second-line biologics compared with those who had secondary loss of response (LOR) or intolerance to the primary therapy, according to a systematic review and meta-analysis presented at the Crohn's & Colitis Congress (CCC) 2018 held recently in Las Vegas, Nevada, US.