Chemical-Genomics Platform Enables Discovery Of Small Molecule ActivatorsOf Numerous Peptide GPCRs
SAN DIEGO, CA and COPENHAGEN, DK, September 26, 2002 - ACADIA Pharmaceuticalsannounced today the discovery of small molecule lead chemistries for the V2Vasopressin receptor. The V2 Vasopressin receptor is the major control mechanismfor the production of urine. Activation of this receptor by ACADIA's lead compoundsresulted in a sustained decrease in urine production in preclinical animal models.
"While V2 peptides that require injection or nasal application have longbeen used to treat diabetes insipidus, bleeding disorders, and nocturnal uresis(bed wetting), an orally active drug may address much broader markets, potentiallyincluding incontinence," said Bo-Ragnar Tolf, Ph.D., ACADIA's Vice Presidentof Chemistry. "ACADIA's small non-peptide molecules have very attractivedrug characteristics and provide us with the potential to develop the firstoral medication that targets V2."
ACADIA's proprietary V2 chemistry is a product of its chemical-genomics efforts.ACADIA is using functional assays to broadly screen the members of the nuclearand G-protein coupled receptor ("GPCR") families, searching for novelchemistries that act as agonist, antagonists, and inverse agonists. More than100 of these targets have been screened, with novel chemistries identified formore than 70 targets. The V2 small molecule chemistry is an example of a non-peptideactivator of a peptide hormone receptor.
"V2 is just one of the examples where we have found exciting small moleculesthat activate peptide GPCRs," said Mark R. Brann, Ph.D., ACADIA's Presidentand CSO. "In the upcoming issue of the Journal of Medicinal Chemistry,we report the structure of our small molecule activator of the Urotensin-IIreceptor, another peptide hormone receptor. We have also discovered the firstsmall molecule activators of the PAR-2 receptor. Our proven ability to consistentlydiscover the first small molecule activators of peptide receptors runs in theface of the pharmaceutical dogma that holds that peptide receptors require complexchemistries that mimic the structure of the natural hormones. The latter areoften referred to as peptoids. Our unique small molecule chemistries have obviouscommercial advantages in terms of bioavailability and future synthetic opportunitiesrelative to the peptides and peptoids."
ACADIA is a drug discovery and development company that efficiently discovers small molecule drug candidates using its proprietary chemical-genomics platform. ACADIA's uniquely productive platform integrates genomics, chemistry and biology to rapidly identify and validate drug targets while simultaneously discovering chemistries specific to those targets. ACADIA has successfully applied its chemical-genomics platform to generate a broad discovery pipeline that includes advanced programs directed at major diseases, including psychosis, chronic pain, and glaucoma. ACADIA's corporate headquarters as well as its genomics and biological research facilities are located in San Diego, California and its chemistry research facilities are located in Copenhagen, Denmark.
Contact:
ACADIA PharmaceuticalsDouglas E. Richards, VP of Business Development+1 858-558-2871
Europe:
Bo-Ragnar Tolf, Ph.D., VP of Chemistry and
Managing Director of ACADIA Pharmaceuticals A/S
+45 4329-3000