Dexloxiglumide Rotta Research Lab.
Dexloxiglumide, the (R)-isomer of loxiglumide, is a selective and highly potent CCK1 receptor antagonist. It is twice as potent as the racemic compound. because the anti-CCK activity is specific to the (R)-form, whereas the (S)-isomer is almost ineffective. It has been developed by Rotta Research Lab SpA for the treatment of diseases in which CCK1 receptor activity is potentially involved, including gastrointestinal motility, food intake and pancreatic disorders [218696]. Its receptor-mediated actions have been described in multiple in vitro and in vivo pharmacological systems. Results from both preclinical and clinical studies indicate that it is an effective inhibitor of gallbladder contraction, improves lower esophegal sphincter (LES) function, accelerates gastric emptying, accelerates colonic transit and significantly decreases symptoms in IBS and functional dyspepsia patients, and therefore has potential as an effective treatment for constipation-predominant IBS. functional dyspesia, constipation, LES function, gastric emptying disorders and biliary colics. Forest Laboratories has entered into an agreement with Rotta for the development and marketing of dexloxiglumide for the treatment of constipation-predominant IBS and phase III studies are currently ongoing in the US. In August 2000, Merrill Lynch expected that dexloxiglumide would not be launched until 2004 [379892], and in June 2001, predicted a US filing date in 2003 [413928].
Varga
Gábor
G
Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest. varga-g@koki.hu
D000818:Animals; D002986:Clinical Trials as Topic; D003109:Colonic Diseases, Functional / Q000188:drug therapy; D004068:Digestive System Physiological Phenomena; D004415:Dyspepsia / Q000188:drug therapy; D016473:Gallbladder Emptying / Q000187:drug effects; D006801:Humans; D010421:Pentanoic Acids / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology*; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*
D010421:Pentanoic Acids; D011949:Receptors, Cholecystokinin; C103490:dexloxiglumide