AI Article Synopsis
- Our research group discovered a new prodrug amino-alcohol that effectively modulates S1P receptors, showing promise as a safer alternative to fingolimod (Gilenya) in terms of lung and heart safety.
- Unlike the marketed drug, this new compound acts as a partial agonist and is expected to have a long half-life in both rodents and humans.
- The purpose of this study is to present these potent S1P partial agonists with shorter half-lives and discuss their pharmacokinetics, pharmacodynamics, and safety assessments in preclinical trials.
Article Abstract
Recently, our research group reported the identification of prodrug amino-alcohol as a potent and efficacious S1P receptor modulator. This molecule is differentiated preclinically over the marketed drug fingolimod (Gilenya ), whose active phosphate metabolite is an S1P full agonist, in terms of pulmonary and cardiovascular safety. S1P partial agonist , however, has a long half-life in rodents and was projected to have a long half-life in humans. The purpose of this communication is to disclose highly potent partial agonists of S1P with shorter half-lives relative to the clinical compound . PK/PD relationships as well as their preclinical pulmonary and cardiovascular safety assessment are discussed.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6071880 | PMC |
| http://dx.doi.org/10.1039/c6md00539j | DOI Listing |
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