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Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Dhar, T G Murali; Xiao, Hai-Yun; Xie, Jenny; Lehman-McKeeman, Lois D; Wu, Dauh-Rurng; Dabros, Marta; Yang, Xiaoxia; Taylor, Tracy L; Zhou, Xia D; Heimrich, Elizabeth M; Thomas, Rochelle; McIntyre, Kim W; Warrack, Bethanne; Shi, Hong; Levesque, Paul C; Zhu, Jia L; Hennan, James; Balimane, Praveen; Yang, Zheng; Marino, Anthony M; Cornelius, Georgia; D'Arienzo, Celia J; Mathur, Arvind; Shen, Ding Ren; Cvijic, Mary Ellen; Salter-Cid, Luisa; Barrish, Joel C; Carter, Percy H; Dyckman, Alaric J.
Affiliation
  • Dhar TG; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Xiao HY; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Xie J; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Lehman-McKeeman LD; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Wu DR; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Dabros M; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Yang X; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Taylor TL; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Zhou XD; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Heimrich EM; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Thomas R; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • McIntyre KW; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Warrack B; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Shi H; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Levesque PC; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Zhu JL; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Hennan J; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Balimane P; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Yang Z; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Marino AM; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Cornelius G; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • D'Arienzo CJ; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Mathur A; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Shen DR; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Cvijic ME; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Salter-Cid L; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Barrish JC; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Carter PH; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
  • Dyckman AJ; Research and Development, Bristol-Myers Squibb Company , Princeton, New Jersey 08543-4000, United States.
ACS Med Chem Lett ; 7(3): 283-8, 2016 Mar 10.
Article de En | MEDLINE | ID: mdl-26985316
ABSTRACT
Clinical validation of S1P receptor modulation therapy was achieved with the approval of fingolimod (Gilenya, 1) as the first oral therapy for relapsing remitting multiple sclerosis. However, 1 causes a dose-dependent reduction in the heart rate (bradycardia), which occurs within hours after first dose. We disclose the identification of clinical compound BMS-986104 (3d), a novel S1P1 receptor modulator, which demonstrates ligand-biased signaling and differentiates from 1 in terms of cardiovascular and pulmonary safety based on preclinical pharmacology while showing equivalent efficacy in a T-cell transfer colitis model.
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Type d'étude: Diagnostic_studies Langue: En Journal: ACS Med Chem Lett Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique
Texte intégral
Ajouter à My VHL
Imprimer
XML
PubMed Links
Recherche sur Google

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Type d'étude: Diagnostic_studies Langue: En Journal: ACS Med Chem Lett Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique