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2008 2
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2011 6
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Page 1
Repositioning of a novel GABA-B receptor agonist, AZD3355 (Lesogaberan), for the treatment of non-alcoholic steatohepatitis.
Bhattacharya D, Becker C, Readhead B, Goossens N, Novik J, Fiel MI, Cousens LP, Magnusson B, Backmark A, Hicks R, Dudley JT, Friedman SL. Bhattacharya D, et al. Sci Rep. 2021 Oct 21;11(1):20827. doi: 10.1038/s41598-021-99008-2. Sci Rep. 2021. PMID: 34675338 Free PMC article.
We used a computational drug repositioning strategy to uncover a novel therapy for NASH, identifying a GABA-B receptor agonist, AZD3355 (Lesogaberan) previously evaluated as a therapy for esophageal reflux. ...In human stellate cells AZD3355 significantly dow …
We used a computational drug repositioning strategy to uncover a novel therapy for NASH, identifying a GABA-B receptor agonist, AZD3355 …
Pharmacokinetic profile of lesogaberan (AZD3355) in healthy subjects: a novel GABA(B)-receptor agonist reflux inhibitor.
Niazi M, Skrtic S, Ruth M, Holmberg AA. Niazi M, et al. Drugs R D. 2011;11(1):77-83. doi: 10.2165/11590310-000000000-00000. Drugs R D. 2011. PMID: 21410297 Free PMC article. Clinical Trial.
BACKGROUND: Lesogaberan (AZD3355) is a novel reflux inhibitor developed as an add-on treatment to proton pump inhibitors (PPIs) for symptom relief in patients with gastroesophageal reflux disease who have a partial response to PPI therapy. OBJECTIVE: The aim of this …
BACKGROUND: Lesogaberan (AZD3355) is a novel reflux inhibitor developed as an add-on treatment to proton pump inhibitors (PPIs …
(R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
Lehmann A, Antonsson M, Holmberg AA, Blackshaw LA, Brändén L, Bräuner-Osborne H, Christiansen B, Dent J, Elebring T, Jacobson BM, Jensen J, Mattsson JP, Nilsson K, Oja SS, Page AJ, Saransaari P, von Unge S. Lehmann A, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12. doi: 10.1124/jpet.109.153593. Epub 2009 Jul 31. J Pharmacol Exp Ther. 2009. PMID: 19648470
AZD3355 and baclofen differed markedly in their distribution in rat brain; AZD3355, but not baclofen, was concentrated in circumventricular organs as a result of active uptake (shown by avid intracellular sequestration) and related to binding of AZD3355 to na …
AZD3355 and baclofen differed markedly in their distribution in rat brain; AZD3355, but not baclofen, was concentrated in circ …
Evaluation of the pharmacokinetic interaction between lesogaberan (AZD3355) and esomeprazole in healthy subjects.
Niazi M, Silberg DG, Miller F, Ruth M, Holmberg AA. Niazi M, et al. Drugs R D. 2010;10(4):243-51. doi: 10.2165/11588180-000000000-00000. Drugs R D. 2010. PMID: 21171670 Free PMC article. Clinical Trial.
BACKGROUND: Transient lower esophageal sphincter relaxations (TLESRs) have been identified as a primary cause of reflux events in patients with gastroesophageal reflux disease (GERD). GABA(B) receptor agonists such as lesogaberan (AZD3355) have been shown to inhibit …
BACKGROUND: Transient lower esophageal sphincter relaxations (TLESRs) have been identified as a primary cause of reflux events in patients w …
A novel reflux inhibitor lesogaberan (AZD3355) as add-on treatment in patients with GORD with persistent reflux symptoms despite proton pump inhibitor therapy: a randomised placebo-controlled trial.
Boeckxstaens GE, Beaumont H, Hatlebakk JG, Silberg DG, Björck K, Karlsson M, Denison H. Boeckxstaens GE, et al. Gut. 2011 Sep;60(9):1182-8. doi: 10.1136/gut.2010.235630. Epub 2011 Mar 14. Gut. 2011. PMID: 21402616 Clinical Trial.
OBJECTIVE: o evaluate the efficacy and tolerability of add-on treatment with lesogaberan (AZD3355), a novel reflux inhibitor, in patients with persistent gastro-oesophageal reflux disease (GORD) symptoms despite proton pump inhibitor (PPI) therapy. ...Lesogaberan …
OBJECTIVE: o evaluate the efficacy and tolerability of add-on treatment with lesogaberan (AZD3355), a novel reflux inhibitor, …
The novel, peripherally restricted GABAB receptor agonist lesogaberan (AZD3355) inhibits acid reflux and reduces esophageal acid exposure as measured with 24-h pHmetry in dogs.
Brändén L, Fredriksson A, Harring E, Jensen J, Lehmann A. Brändén L, et al. Eur J Pharmacol. 2010 May 25;634(1-3):138-41. doi: 10.1016/j.ejphar.2010.02.015. Epub 2010 Feb 20. Eur J Pharmacol. 2010. PMID: 20176012
The GABAB receptor agonist baclofen inhibits transient LES relaxation but it is not an ideal agent due to central nervous system activity. Lesogaberan (AZD3355) is a peripherally restricted GABAB receptor agonist with limited central nervous system activity that inh …
The GABAB receptor agonist baclofen inhibits transient LES relaxation but it is not an ideal agent due to central nervous system activity. …
Efficacy and safety of pharmacotherapy for refractory or unexplained chronic cough: a systematic review and network meta-analysis.
Zheng Z, Huang J, Xiang Z, Wu T, Lan X, Xie S, Lin Z, Tang K, Morice A, Li S, Song WJ, Chen R. Zheng Z, et al. EClinicalMedicine. 2023 Jul 20;62:102100. doi: 10.1016/j.eclinm.2023.102100. eCollection 2023 Aug. EClinicalMedicine. 2023. PMID: 37538538 Free PMC article.
In the network meta-analysis, gefapixant is the most effective treatment for patients with RCC (The Surface Under the Cumulative Ranking Curves (SUCRA) is 0.711 in LCQ, 0.983 in 24 h cough frequency, and 0.786 in cough severity VAS). Lesogaberan had better efficacy than pl …
In the network meta-analysis, gefapixant is the most effective treatment for patients with RCC (The Surface Under the Cumulative Ranking Cur …
Management of refractory typical GERD symptoms.
Scarpellini E, Ang D, Pauwels A, De Santis A, Vanuytsel T, Tack J. Scarpellini E, et al. Nat Rev Gastroenterol Hepatol. 2016 May;13(5):281-94. doi: 10.1038/nrgastro.2016.50. Epub 2016 Apr 14. Nat Rev Gastroenterol Hepatol. 2016. PMID: 27075264 Review.
GABAB receptor agonism as a novel therapeutic modality in the treatment of gastroesophageal reflux disease.
Lehmann A, Jensen JM, Boeckxstaens GE. Lehmann A, et al. Adv Pharmacol. 2010;58:287-313. doi: 10.1016/S1054-3589(10)58012-8. Adv Pharmacol. 2010. PMID: 20655487 Review.
In this article we review the in vitro and in vivo pharmacology of the peripherally-restricted GABA(B) receptor agonists and the preclinical and clinical development of lesogaberan (AZD3355, (R)-(3-amino-2-fluoropropyl) phosphinic acid), a potent and predominately p …
In this article we review the in vitro and in vivo pharmacology of the peripherally-restricted GABA(B) receptor agonists and the preclinical …
Repurposing Lesogaberan to Promote Human Islet Cell Survival and beta-Cell Replication.
Tian J, Dang H, Hu A, Xu W, Kaufman DL. Tian J, et al. J Diabetes Res. 2017;2017:6403539. doi: 10.1155/2017/6403539. Epub 2017 Sep 5. J Diabetes Res. 2017. PMID: 29018828 Free PMC article.
This study tested the hypothesis that lesogaberan could be repurposed to promote human islet cell survival and beta-cell replication. ...Lesogaberan may be a promising drug candidate for clinical studies of diabetes intervention and islet transplantation....
This study tested the hypothesis that lesogaberan could be repurposed to promote human islet cell survival and beta-cell replication. …
39 results