Eluxadoline, also known as JNJ-27018966, is a novel, orally-active drug approved for the treatment of diarrhea and abdominal pain in individuals with diarrhea-predominant irritable bowel syndrome (IBS-D). It was approved for use by the United States Food and Drug Administration on May 27, 2015. Eluxadoline is a μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist that acts locally in the enteric nervous system, possibly decreasing adverse effects on the central nervous system. This product is discintinued (DEA Schedule IV).
Reference: Anon. Crystalline forms of methyl 5-(((S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-((S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoate dihydrochloride. Volume 16. Issue 4A. Pages 1-3. (Journal; Patent)
Anon. Crystalline forms of methyl 5-(((S)-2-amino-3-(4-carbamoyl-2,6-dimethylphenyl)-N-((S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl)propanamido)methyl)-2-methoxybenzoate dihydrochloride. Volume 16. Issue 4A. Pages 1-3. (Journal; Patent)
Reference: Anon. Process for the preparation of (S)-2-((tert-butoxycarbonyl) amino)-3-(4-carbamoyl-2,6 dimethylphenyl) propanoic acid. Volume 15 Issue 11A Pages 1pp.(Journal; Patent)
Anon. Process for the preparation of (S)-2-((tert-butoxycarbonyl) amino)-3-(4-carbamoyl-2,6 dimethylphenyl) propanoic acid. Volume 15 Issue 11A Pages 1pp.(Journal; Patent)
Reference: Inamdar, Murad Ismail; Mohan, Sriram Hari; Hirpara, Ketan Vithalbhai. Processes for the preparation of eluxadoline. WO 2018055528. (Assignee Sun Pharmaceutical Industries Limited, India)
Inamdar, Murad Ismail; Mohan, Sriram Hari; Hirpara, Ketan Vithalbhai. Processes for the preparation of eluxadoline. WO 2018055528. (Assignee Sun Pharmaceutical Industries Limited, India)
Reference: Chen, Minhua; Zhang, Yanfeng; Liu, Kai; Lu, Fei; Ji, Shulin; Zhang, Liang; Yang, Chaohui. New crystal form of eluxadoline and preparation method thereof. WO 2017114446. (Assignee Crystal PharmaTech Co., Ltd., Peop. Rep. China)
Chen, Minhua; Zhang, Yanfeng; Liu, Kai; Lu, Fei; Ji, Shulin; Zhang, Liang; Yang, Chaohui. New crystal form of eluxadoline and preparation method thereof. WO 2017114446. (Assignee Crystal PharmaTech Co., Ltd., Peop. Rep. China)
Reference: Rajan, Srinivasan Thirumalai; Eswaraiah, Sajja; Reddy, Sagyam Rajeshwar; Prabhakar, Macharla; Rajesham, Boge. Process for the preparation of 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4 -phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid and its polymorphs. WO 2017191650. (Assignee MSN Laboratories Private Limited, India)
Rajan, Srinivasan Thirumalai; Eswaraiah, Sajja; Reddy, Sagyam Rajeshwar; Prabhakar, Macharla; Rajesham, Boge. Process for the preparation of 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4 -phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid and its polymorphs. WO 2017191650. (Assignee MSN Laboratories Private Limited, India)
Mawale, Vishal Sukhadeo; Mahakal, Kumodini Kashinath; Mahajan, Pravin Raghunath; Singh, Gurvinder Pal; Ray, Purna Chandra; Singh, Girij Pal; Rajput, Lalitkumar Dilipsing; Shivdavkar, Radhakrishna Bhikaji. Process for the preparation of Eluxadoline. Assignee Lupin Limited, India. WO 2018020450. 2018.
