Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
ACS Med Chem Lett
; 7(3): 283-8, 2016 Mar 10.
Artigo
em Inglês
| 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.
Texto completo:
Disponível
Coleções:
Bases de dados internacionais
Base de dados:
MEDLINE
Idioma:
Inglês
Revista:
ACS Med Chem Lett
Ano de publicação:
2016
Tipo de documento:
Artigo
País de afiliação:
Estados Unidos
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