Endothelial-protective effects of a G-protein-biased sphingosine-1 phosphate receptor-1 agonist, SAR247799, in type-2 diabetes rats and a randomized placebo-controlled patient trial.
Luc BergougnanGrit AndersenLeona Plum-MörschelMaria Francesca EvaristiBruno PoirierAgnes TardatMarcel ErmerTheresa HerbrandJorge ArrublaHans Veit CoesterRoberto SansoneChristian HeissOlivier VitseFabrice HurbinRania BoironXavier BenainDavid RadzikPhilip JaniakAnthony J MuslinLionel HovsepianStephane KirkesseliPaul DeutschAshfaq A ParkarPublished in: British journal of clinical pharmacology (2020)
These data provide the first human evidence suggesting endothelial-protective properties of S1P1 activation, with SAR247799 being as effective as the clinical benchmark, sildenafil. Further clinical testing of SAR247799, at sub-lymphocyte-reducing doses (≤5 mg), is warranted in vascular diseases associated with endothelial dysfunction.
Keyphrases
- endothelial cells
- type diabetes
- study protocol
- phase iii
- placebo controlled
- clinical trial
- cardiovascular disease
- phase ii
- electronic health record
- randomized controlled trial
- pulmonary hypertension
- double blind
- machine learning
- squamous cell carcinoma
- glycemic control
- insulin resistance
- big data
- skeletal muscle
- adipose tissue
- open label