ACADIA Pharmaceuticals Inc., a biopharmaceutical company utilising innovative technology to fuel drug discovery and clinical development of novel treatments for central nervous system disorders, has discovered a novel isoform-selective retinoic acid receptor (RAR) agonists and a highly effective hit-to-lead optimisation providing RARb2 agonists with drug-like properties. The published compounds may serve as pharmacological tools to further explore nuclear receptor pharmacology and may provide a starting point for drug development efforts.

"The discovery of novel isoform-selective RAR agonists demonstrates the high quality and broad applicability of ACADIA's drug discovery engine. We will continue to leverage our proprietary assay technology to augment our pipeline of drug candidates to treat CNS disorders and other areas of unmet medical need," said Mark Brann, ACADIA's president and chief scientific officer.

According to a company release, an ultra high-throughput screen of RAR subtypes was performed using ACADIA's proprietary R-SAT technology. Although the initial hit did not display drug-like properties and previously had been studied only in the context of liquid crystal technology, ACADIA scientists succeeded in optimising the structure of the agonists into small molecules with retained potency, selectivity, and favourable drug-like properties. In initial pharmacological studies, these novel selective agonists showed cellular effects consistent with a retinoid-like mode of action.

RARs belong to the steroid family of nuclear hormone receptors.

ACADIA is a biopharmaceutical company utilising innovative technology to fuel drug discovery and clinical development of novel treatments for central nervous system disorders.