molecules of the month


G-protein biased GPCR agonist

oral 10 mg QD, phase I, cardiovascular

from HTS and opt.



Chemical structure of SAR247799
1 min read

The Sanofi S1P1 agonist, SAR247799, is a biased agonist of the S1P1 sphingosine receptor, preferentially activating G-protein signaling over the β-arrestin and internalization pathways. Commercial S1P1 modulators such as fingolimod and ozanimod exert their immunosuppressive effects in multiple sclerosis and other diseases primarily by downregulating the S1P1 receptor through agonism and receptor internalization. Through biased agonism, SAR247799 exhibits a variety of endothelial-protective properties without reducing lymphocytes in a number of animal models, including a pig coronary microvascular hyperemic response model. SAR247799 demonstrates good safety and tolerability in healthy subjects (and improves endothelial function, as assessed by flow-mediated dilation in type-2 diabetic patients (NCT03462017). This is likely an important clinical study for the biased agonism field, which has recently been challenged by the…

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