Table 3.
Comparison of secretagogues, lubiprostone and linaclotide
| Lubiprostone | Linaclotide | |
|---|---|---|
| Chemistry | Bicyclic fatty acid called a prostone | 14 amino acid peptide, analogue of guanylin |
| Target receptor | Chloride channel (ClC2); ? CFTR involved | Guanylate cyclase C receptor activation with CFTR-mediated secretion |
| Pharmacodynamics in humans | Accelerated small bowel and colonic transit in health | Accelerated colonic transit in IBS-C in dose-related fashion |
| Clinical trial efficacy | Phase II and III portfolio in chronic constipation and C-IBS | Phase IIB in chronic constipation and IBS-C |
| Open label effectiveness | Clinical practice experience | – |
| Arrhythmogenicity | No arrhythmic activity | Low bioavailability, no arrhythmic activity |
| Cardiovascular safety | Healthy subjects 'thorough' QTc study | Healthy subjects 'thorough' QTc study |
| Commonest AEs | Diarrhoea, nausea | Diarrhoea |
| Potential other actions | Mucosal protection | Anti-neoplastic |
| Approval status | FDA | – |