Revexepride

• CAT Number: I009018
• CAS Number: 219984-49-3
• Molecular Formula: C21H32ClN3O4
• Molecular Weight: 425.954
• Purity: ≥95%
• Target: 5-HT4 receptor agonist
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• InChI: InChI=1S/C21H32ClN3O4/c1-21(2)10-15-18(23)16(22)9-14(19(15)29-21)20(27)24-11-13-5-7-25(12-17(13)26)6-4-8-28-3/h9,13,17,26H,4-8,10-12,23H2,1-3H3,(H,24,27)/t13-,17+/m0/s1
• InChIKey: FOUUNSGQVBGYQM-SUMWQHHRSA-N
• SMILES: O=C(C1=CC(Cl)=C(N)C2=C1OC(C)(C)C2)NC[C@H]3[C@H](O)CN(CCCOC)CC3

Revexepride (Cat.No:I009018), also known as SSP-002358, is a 5-HT4 receptor agonist and a novel prokinetic that stimulates gastrointestinal motility, which has been suggested as a continued cause of symptoms in these patients. Clinical trials showed that revexepride was no more effective than placebo in controlling regurgitation in patients with GERD symptoms partially responsive to PPIs. Revexepride was well tolerated.

Reference

1:Pharmacokinetics, absorption, and excretion of radiolabeled revexepride: a Phase I clinical trial using a microtracer and accelerator mass spectrometry-based approach. Flach S, Croft M, Ding J, Budhram R, Pankratz T, Pennick M, Scarfe G, Troy S, Getsy J.Drug Des Devel Ther. 2016 Sep 27;10:3125-3132. eCollection 2016. PMID: 27729771 Free PMC Article2:Randomized clinical trial: a controlled pilot trial of the 5-HT4 receptor agonist revexepride in patients with symptoms suggestive of gastroparesis. Tack J, Rotondo A, Meulemans A, Thielemans L, Cools M.Neurogastroenterol Motil. 2016 Apr;28(4):487-97. doi: 10.1111/nmo.12736. PMID: 27010235 3:A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults. Pierce D, Corcoran M, Velinova M, Hossack S, Hoppenbrouwers M, Martin P.Drug Des Devel Ther. 2015 Feb 27;9:1257-68. doi: 10.2147/DDDT.S64621. eCollection 2015. PMID: 25767373 Free PMC Article4:Randomised clinical trial: the 5-HT4 agonist revexepride in patients with gastro-oesophageal reflux disease who have persistent symptoms despite PPI therapy. Shaheen NJ, Adler J, Dedrie S, Johnson D, Malfertheiner P, Miner P, Meulemans A, Poole L, Tack J, Thielemans L, Troy S, Vakil N, Zerbib F, Ruth M.Aliment Pharmacol Ther. 2015 Apr;41(7):649-61. doi: 10.1111/apt.13115. Epub 2015 Feb 19. PMID: 25693609 Free PMC Article5:Randomized clinical trial: effect of the 5-HT4 receptor agonist revexepride on reflux parameters in patients with persistent reflux symptoms despite PPI treatment. Tack J, Zerbib F, Blondeau K, des Varannes SB, Piessevaux H, Borovicka J, Mion F, Fox M, Bredenoord AJ, Louis H, Dedrie S, Hoppenbrouwers M, Meulemans A, Rykx A, Thielemans L, Ruth M.Neurogastroenterol Motil. 2015 Feb;27(2):258-68. doi: 10.1111/nmo.12484. Epub 2014 Dec 21. PMID: 25530111 Free PMC Article