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2011 2
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2018 3
2019 2
2023 0
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Page 1
Efficacy of Treatments for Opioid-Induced Constipation: Systematic Review and Meta-analysis.
Nee J, Zakari M, Sugarman MA, Whelan J, Hirsch W, Sultan S, Ballou S, Iturrino J, Lembo A. Nee J, et al. Clin Gastroenterol Hepatol. 2018 Oct;16(10):1569-1584.e2. doi: 10.1016/j.cgh.2018.01.021. Epub 2018 Jan 31. Clin Gastroenterol Hepatol. 2018. PMID: 29374616
Approved treatments for OIC are methylnaltrexone, naloxone, naloxegol, alvimopan, naldemedine, and lubiprostone. Since a meta-analysis performed in 2014, 2 new agents have been approved by the Food and Drug Administration for treatment of OIC (naloxegol and naldemedine). . …
Approved treatments for OIC are methylnaltrexone, naloxone, naloxegol, alvimopan, naldemedine, and lubiprostone. Since a meta-analysis perfo …
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
Long DD, Armstrong SR, Beattie DT, Campbell CB, Church TJ, Colson PJ, Dalziel SM, Jacobsen JR, Jiang L, Obedencio GP, Rapta M, Saito D, Stergiades I, Tsuruda PR, Van Dyke PM, Vickery RG. Long DD, et al. ACS Med Chem Lett. 2019 Nov 26;10(12):1641-1647. doi: 10.1021/acsmedchemlett.9b00406. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857840 Free PMC article.
Herein, we describe the application of Theravance's multivalent approach to drug discovery coupled with a physicochemical property design strategy by which the N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenyl carbo …
Herein, we describe the application of Theravance's multivalent approach to drug discovery coupled with a physicochemical property design st …
Novel Oral Therapies for Opioid-induced Bowel Dysfunction in Patients with Chronic Noncancer Pain.
Holder RM, Rhee D. Holder RM, et al. Pharmacotherapy. 2016 Mar;36(3):287-99. doi: 10.1002/phar.1711. Epub 2016 Mar 6. Pharmacotherapy. 2016. PMID: 26945548 Review.
Lubiprostone and naloxegol are approved in the United States by the Food and Drug Administration for use in opioid-induced constipation. Axelopran (TD-1211) and sustained-release naloxone have undergone phase 2 and phase 1 studies, respectively, …
Lubiprostone and naloxegol are approved in the United States by the Food and Drug Administration for use in opioid-induced constipation. …
The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist.
Tsuruda PR, Vickery RG, Long DD, Armstrong SR, Beattie DT. Tsuruda PR, et al. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):479-91. doi: 10.1007/s00210-013-0850-7. Epub 2013 Apr 4. Naunyn Schmiedebergs Arch Pharmacol. 2013. PMID: 23549670
TD-1211 bound with high affinity to human recombinant mu and delta, and guinea pig kappa receptors expressed in CHO-K1 cells (pK d = 9.7, 8.6, and 9.9, respectively). ...Functionally, TD-1211 behaved as an antagonist at all three receptor types
TD-1211 bound with high affinity to human recombinant mu and delta, and guinea pig kappa receptors expressed in CHO-K1 cells (
The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity.
Armstrong SR, Campbell CB, Richardson CL, Vickery RG, Tsuruda PR, Long DD, Hegde SS, Beattie DT. Armstrong SR, et al. Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun;386(6):471-8. doi: 10.1007/s00210-013-0844-5. Epub 2013 Mar 13. Naunyn Schmiedebergs Arch Pharmacol. 2013. PMID: 23512167
The oral activity of TD-1211 was evaluated in models of gastrointestinal (GI) and central nervous system (CNS) function in the rat and dog. ...The data from these studies support the clinical development of TD-1211 as a novel treatment for opioid-induc …
The oral activity of TD-1211 was evaluated in models of gastrointestinal (GI) and central nervous system (CNS) function in the …
Opioid-induced constipation: challenges and therapeutic opportunities.
Camilleri M. Camilleri M. Am J Gastroenterol. 2011 May;106(5):835-42; quiz 843. doi: 10.1038/ajg.2011.30. Epub 2011 Feb 22. Am J Gastroenterol. 2011. PMID: 21343919 Review.
Several different pharmacological approaches are being developed to prevent or treat OIC: prolonged release formulations that contain naloxone (a less specific opiate antagonist that is widely distributed) and a new class of peripherally restricted mu-opiate receptor antagonists, …
Several different pharmacological approaches are being developed to prevent or treat OIC: prolonged release formulations that contain naloxo …
New developments in the treatment of opioid-induced gastrointestinal symptoms.
Pannemans J, Vanuytsel T, Tack J. Pannemans J, et al. United European Gastroenterol J. 2018 Oct;6(8):1126-1135. doi: 10.1177/2050640618796748. Epub 2018 Aug 27. United European Gastroenterol J. 2018. PMID: 30288274 Free PMC article. Review.
Efficacy data for laxatives, lubiprostone, prucalopride, linaclotide, oxycodone/naloxone combinations, methylnaltrexone, alvimopan, naloxegol, naldemedine, axelopran, and bevenopran in OIC are summarised....
Efficacy data for laxatives, lubiprostone, prucalopride, linaclotide, oxycodone/naloxone combinations, methylnaltrexone, alvimopan, naloxego …
Discovery of N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists.
Jiang L, Beattie DT, Jacobsen JR, Kintz S, Obedencio GP, Saito D, Stergiades I, Vickery RG, Long DD. Jiang L, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2926-2930. doi: 10.1016/j.bmcl.2017.04.092. Epub 2017 May 3. Bioorg Med Chem Lett. 2017. PMID: 28499731
Second generation therapies target a localized, peripherally-restricted, non-CNS penetrant drug distribution of opioid receptor antagonists. Herein we describe the discovery of the N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3- …
Second generation therapies target a localized, peripherally-restricted, non-CNS penetrant drug distribution of opioid receptor antagonists. …
Investigational opioid antagonists for treating opioid-induced bowel dysfunction.
Mozaffari S, Nikfar S, Abdollahi M. Mozaffari S, et al. Expert Opin Investig Drugs. 2018 Mar;27(3):235-242. doi: 10.1080/13543784.2018.1420778. Epub 2017 Dec 26. Expert Opin Investig Drugs. 2018. PMID: 29266973 Review.
AREAS COVERED: Clinical evidence for investigational PAMORAs was reviewed and clinical trials on investigational agents to reduce OIC were included. TD-1211 is currently being evaluated in Phase II clinical trial. ...
AREAS COVERED: Clinical evidence for investigational PAMORAs was reviewed and clinical trials on investigational agents to reduce OIC were i …
Clinical Overview and Considerations for the Management of Opioid-induced Constipation in Patients With Chronic Noncancer Pain.
Viscusi ER. Viscusi ER. Clin J Pain. 2019 Feb;35(2):174-188. doi: 10.1097/AJP.0000000000000662. Clin J Pain. 2019. PMID: 30289777 Free PMC article. Review.
Prescription medications are indicated when OIC persists despite conservative approaches (eg, increased fiber and fluid intake, exercise, over-the-counter laxatives and stool softeners). Phase 3 studies have demonstrated the efficacy of peripherally acting -opioid receptor …
Prescription medications are indicated when OIC persists despite conservative approaches (eg, increased fiber and fluid intake, exercise, ov …
11 results