Acadia says research published on isoform-selective retinoic acid receptors, may lead to drugs

By E. Janene Geiss

Philadelphia, Dec. 15 - Acadia Pharmaceuticals Inc. announced Thursday the publication of research in both the Journal of Medicinal Chemistry and in Biochemical Pharmacology that reports Acadia's discovery of novel isoform-selective retinoic acid receptor (RAR) agonists and a highly effective hit-to-lead optimization 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, according to a company news release.

"The discovery of novel isoform-selective RAR agonists demonstrates the high quality and broad applicability of Acadia's drug discovery engine," Mark Brann, president and chief scientific officer, said in the release.

"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," Brann said.

The Journal of Medicinal Chemistry and the Biochemical Pharmacology articles describe research conducted by Acadia scientists that led to the discovery of novel isoform-selective RARb2 agonists.

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 said its scientists succeeded in optimizing the structure of the agonists into small molecules with retained potency, selectivity and favorable drug-like properties.

In initial pharmacological studies, these novel selective agonists showed cellular effects consistent with a retinoid-like mode of action, officials said.

Acadia is a San Diego biopharmaceutical company utilizing innovative technology to fuel drug discovery and clinical development of novel treatments for central nervous system disorders.

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