June 13, 2002 - General
SAN DIEGO, CA, June 13, 2002 – ACADIA Pharmaceuticals announced thesuccessful application of its proprietary chemical-genomics approach to morethan 100 G-protein coupled receptor (“GPCR”) and nuclear receptor targets. Thepresentation was made by Mark R. Brann, Ph.D., ACADIA's President andChief Scientific Officer, at the Chemical Genomics Session of the 28th NationalMedicinal Chemistry Symposium in San Diego, California. ACADIA reported thatits discovery efforts to date have resulted in the identification of novelsmall molecule ligands for over 60 of these targets, including agonists forseveral targets previously believed to be non-druggable.
Chemical genomics is an emerging, highly productive approach to drug discoverywhere novel chemistries are systematically sought for a diversity of targets inlarge gene families. Identified specific chemistries are used as critical toolsto help elucidate the therapeutic potential of these targets. Equallyimportant, once functionally relevant and drug-like chemistries are discoveredfor a given target, efficient lead optimization efforts may be rapidlyinitiated.
ACADIA's chemical genomics efforts have focused on two gene families that areparticularly rich in drug targets, the GPCRs and nuclear receptors. Together,these two important gene families are believed to be the targets of more thanhalf of the known drugs. ACADIA has established functional assays for more than250 targets out of the approximately 500 GPCRs and nuclear receptors within itschemical-genomics platform. To date, ACADIA has applied its chemical-genomicsapproach to over 100 of these targets, and has successfully identified novelsmall molecule chemistries for more than 60 targets.
“It is very exciting to compare the chemistries for such a diversity oftargets,” said Mark R. Brann, Ph.D., ACADIA's President and ChiefScientific Officer. “This approach has provided ACADIA with a wealth ofopportunities for drug discovery programs and has already led to several drugcandidates rapidly approaching the clinic. In addition, we have identified thefirst ligands for several unexploited targets that provide us with new andexciting program opportunities. Two particularly interesting examples are smallmolecule agonists for HNF4a is an orphan nuclear receptor that when mutated causes MODY, a form of diabetesmellitus. While HNF4a is an exquisitely well-validated target, the pharmaceutical industry has notreported suitable small molecule chemistries for this target. PAR2 is a GPCRthat is activated by the protease trypsin. Many lines of evidence point to arole of this receptor in inflammatory disease and neuropathic pain. Theseexciting discoveries position ACADIA to launch the first small molecule drugdiscovery efforts aiming at innovative therapies that exploit HNF4a and PAR2 modulation.”
ACADIA has used its chemical-genomics platform to generate a broad drugdiscovery pipeline that addresses large unmet medical needs and majorcommercial markets, including psychosis. “Our inverse agonist for the 5HT2Areceptor, ACP-103, is scheduled to enter clinical trials later this year,” saidRobert E. Davis, Ph.D., ACADIA's Executive Vice President of Drug Discovery andDevelopment. “In this program, we used our chemical-genomics platform torapidly identify compounds with the desired combination of potency, specificityand efficacy for use as antipsychotics. In our muscarinic m1 psychosis program,our platform enabled the discovery of highly specific chemistries that interactwith a unique ‘ectopic' binding site on the m1 receptor. This discovery led toa program now in late-stage preclinical testing, which positions ACADIA toexploit the therapeutic opportunities afforded by the first truly selective m1agonist.”
ACADIA is a drug discovery and development company that efficiently discoverssmall molecule drug candidates using its proprietary chemical-genomicsplatform. ACADIA's uniquely productive platform integrates genomics, chemistryand biology to rapidly identify and validate drug targets while simultaneouslydiscovering chemistries specific to those targets. ACADIA has successfullyapplied its chemical-genomics platform to generate a broad discovery pipelinethat includes advanced programs directed at major diseases, includingpsychosis, chronic pain, and glaucoma. ACADIA's corporate headquarters as wellas its genomics and biological research facilities are located in San Diego,California and its chemistry research facilities are located in Copenhagen,Denmark.
Contact:
ACADIA Pharmaceuticals
Mark R. Brann, Ph.D., President and CSO
Douglas E. Richards, VP of Business Development
+1 858 558 2871