Discovery of First Small Molecule Agonists for NPFF and MrG Receptors
SAN DIEGO, CA, December 10, 2002 - ACADIA Pharmaceuticals announcedtoday the discovery of the first small molecule chemistries that activate twoimportant G-protein coupled receptor (GPCR) targets, the NPFF and the MrG receptors.Small molecule drugs acting on these recently discovered targets represent apotential breakthrough in the treatment of pain. ACADIA's novel lead chemistriesbroaden the Company's therapeutic pain portfolio, which also includes ACP-102,a GPCR agonist that is scheduled to enter clinical development shortly for thetreatment of neuropathic pain in cancer patients, and preclinical compoundsthat target a specific subtype of the muscarinic receptors.
NPFF and MrG receptors are members of the family of gene products referredto as GPCRs. This family represents the targets of a diversity of blockbusterdrugs and genomic efforts have shown the existence of more than 400 pharmaceuticallyrelevant GPCRs. Most of these GPCRs have no known hormones or chemistries thatactivate them, and are referred to as "orphan" receptors. NPFF receptorsare prominently expressed in the spinal cord where they mediate the analgesicresponses of the peptide NPFF. Recently, NPFF was found to activate one of theorphan receptors present in the spinal cord. The MrG receptors are orphan GPCRsthat are exclusively expressed by the neurons in the dorsal root ganglia thattransmit pain signals to the central nervous system.
"To our knowledge, we have discovered the first small molecule chemistriesthat activate these targets," said Mark R. Brann, Ph.D., ACADIA's Presidentand Chief Scientific Officer. "The chemistries are potent, selective anddrug-like. In the case of the MrGs we have a range of chemistries that differentiateamong the subtypes. It is very exciting to launch drug discovery programs incompletely new areas where the biology is so compelling." These chemistrieswere initially found through ACADIA's chemical-genomics approach, where ACADIAis systematically screening members of the GPCR gene family in the search fornovel chemistries. To date the approach has been applied to more than 100 GPCRs,and novel chemistries have been identified for more than 60 of these targets.
"These targets and chemistries expand our drug discovery efforts in paintherapeutics," said Robert E. Davis, Ph.D., ACADIA's Executive Vice Presidentof Drug Discovery and Development. "We have two other pain programs: ACP-102that also targets a GPCR and our advanced preclinical program that exploitsmuscarinic receptors. We have the necessary preclinical models and developmentcapabilities to rapidly push these new opportunities forward."
ACADIA Pharmaceuticals is a drug discovery and development company that efficientlydiscovers small molecule drug candidates using its proprietary chemical-genomicsplatform. ACADIA has successfully applied its platform to generate a broad discoverypipeline that includes advanced programs directed at major diseases, includingParkinson's disease, psychosis, chronic pain, and glaucoma. ACADIA's corporateheadquarters as well as its genomics and biological research facilities arelocated in San Diego, California and its chemistry research facilities are locatedin Copenhagen, Denmark.
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