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Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
Tegaserod is a promotility agent, which acts as an agonist at serotonin type 4(5-HT4) receptors in the GI tract. It normalizes impaired motility in the GI tract, inhibits visceral sensitivity, and stimulates intestinal secretion. Tegaserod is approved by the Food and Drug Administration (FDA) for short-term treatment only of constipation-predominant irritable bowel syndrome in patients below 65 years of age. Its use in palliative care patients has not been investigated.
Pathophysiology and Management of Diabetic Gastropathy
Published in Emmanuel Opara, NUTRITION and DIABETES, 2005
Tegaserod is a serotonergic (5-HT4) receptor partial agonist and has been approved by the FDA for treatment of women with constipation-predominant irritable-bowel syndrome.149 Although it increases orocecal transit time with preliminary promising results on gastric emptying, further studies are needed to determine its role in the management of gastroparesis.150–152 Use of tegaserod has been associated in routine medical care with the development of diarrhea, and possibly ischemic colitis.
Abdominal Pain
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Tegaserod was released in July 2002 and is FDA-approved for the treatment of constipation-predominant IBS (IBS-C). Tegaserod is a 5-HT4 receptor agonist, which is involved in the peristaltic action of the gut (Lacy, 2002). Large randomized controlled studies have been done using tegaserod and have demonstrated significant global symptom improvement (pain, bloating) in addition to relieving constipation problems. Nearly two thirds of women studied had improvement or resolution of IBS-C related symptoms (Brandt et al., 2002; Lacy, 2002; Muller-Lissner et al., 2001; Prather et al., 2000). At the current time, tegaserod is approved only for use in women, but studies showing efficacy in men with IBS-C are currently in progress. In April 2004, Novartis, makers of Zelnorm, released a statement warning physicians of the dangers of diarrhea that can be induced by the medication and rare case reports of ischemic colitis. All potential serious adverse events are to be reported to the FDA MEDWATCH program.
Emerging therapies in the management of Irritable Bowel Syndrome (IBS)
Published in Expert Opinion on Emerging Drugs, 2022
Jill E. Elwing, Hadi Atassi, Benjamin D. Rogers, Gregory S. Sayuk
Tegaserod is a 5-HT4 agonist that functions as a prokinetic and recently was reapproved for use in the management of IBS-C patients. Tegaserod was first approved by the FDA in 2002, but later was voluntarily withdrawn from the market in 2007 over concerns relating to increased cardiovascular risk. It was once again reapproved in 2019 with a more restricted patient population of women under the age of 65 without a history of cardiovascular disease and ≤ 1 cardiovascular risk factor (e.g. obesity, diabetes hypertension, hyperlipidemia, tobacco use). Two independent, external adjudications of tegaserod clinical trial data (18,645 patients) found tegaserod to be safe in this indicated female population [36]. The original phase 3 trials demonstrating efficacy relied on a ‘subjective global assessment’ endpoint wherein patients endorsed ‘considerable’ or ‘complete’ relief ≥ 50% of study weeks or at least ‘somewhat relieved’ 100% of weeks 8–12 in the study. Reanalysis of the clinical trial data using contemporary FDA endpoints suggested that tegaserod achieved this outcome to a statistically greater level than placebo (36.0% vs. 24.3%, P < 0.001) [37]. Despite a more restricted patient population, additional analyses suggest a similar potential for symptom response and side effects in this indicated population [37]. ACG Guidelines make a conditional recommendation for tegaserod use based on low quality of evidence [3].
Therapeutic modulators of the serotonin 5-HT4 receptor: a patent review (2014-present)
Published in Expert Opinion on Therapeutic Patents, 2020
Caroline Lanthier, Patrick Dallemagne, Cédric Lecoutey, Sylvie Claeysen, Christophe Rochais
If selective 5-HT4R antagonists have been proposed to treat atrial fibrillation or irritable bowel syndrome (IBS) [3], most of the efforts were put to develop agonists. Agonists display potent prokinetic properties, enhance intestinal peristalsis and gastric emptying, and decrease esophageal reflux, but were often linked to non-target mediated toxicity [4]. Among them, Cisapride 1 was known to interact with hERG channels (Table 1) [5]. This derivative is representative of the aminobenzamide scaffold which has been explored in a number of other compounds presented in the manuscript. Tegaserod 2 was firstly approved by the FDA in 2002 to treat the constipation associated with IBS in women [6]. Tegaserod was however withdrawn in 2007 due to cardiac adverse effects linked to prolonged QT interval. Conversely, a large cohort study ‘found no evidence for an increased risk of cardiovascular ischemic events in Tegaserod users’ [7]. Tegaserod was then reintroduced in March 2019 after a complete safety review by the FDA [8]. Prucalopride 3, a highly selective 5-HT4R agonist, approved by the FDA in 2018 to treat chronic idiopathic constipation by enhancing colon peristalsis and increasing bowel motility, appears also to be devoid of cardiac risk [9]. This is also the case for Minesapride 4 (Figure 1) that was also proved to be devoid of any QT prolongation [10].
Current and emerging therapeutic options for the management of functional dyspepsia
Published in Expert Opinion on Pharmacotherapy, 2020
A. Vandenberghe, J. Schol, K. Van den Houte, I. Masuy, F. Carbone, J. Tack
Tegaserod is a partial 5-HT4 agonist indicated in constipation-predominant irritable bowel syndrome (IBS-C) and functional constipation. It was also evaluated in FD [32,37,49,50]. The phase 2b program showed that 6-mg b.i.d were efficacious in females suffering from moderate and severe meal-related FD symptoms, a patient description reminiscent of what later would become PDS according to Rome III [1,49]. Both pivotal phase 3 trials failed to confirm these results, although one of the studies was statistically significant [50]. The main reason is probably a change in patient selection criteria compared to phase 2b and especially the inclusion of patients with only mild symptoms whose response to drug was not superior over placebo [50]. As for Itopride Tegaserod, 6 mg deserves to be assessed in PDS patients according to the Rome IV criteria and using a validated instrument.