ACADIA Applies Chemical Genomics to Discover Small Molecule
Leads For Numerous GPCRs and Nuclear Receptors
Proprietary Platform Has Identified Novel Chemistries for Over 60 Targets Including the First Agonists for HNF4-alpha and PAR2
2002-06-13 06:01 (New York)
SAN DIEGO, June 13 /PRNewswire/ -- ACADIA Pharmaceuticals announced the
successful application of its proprietary chemical-genomics approach to more
than 100 G-protein coupled receptor ("GPCR") and nuclear receptor targets.
The presentation was made by Mark R. Brann, Ph.D., ACADIA's President and
Chief Scientific Officer, at the Chemical Genomics Session of the 28th
National Medicinal Chemistry Symposium in San Diego, California. ACADIA
reported that its discovery efforts to date have resulted in the
identification of novel small molecule ligands for over 60 of these targets,
including agonists for several targets previously believed to be
non-druggable.
Chemical genomics is an emerging, highly productive approach to drug
discovery where novel chemistries are systematically sought for a diversity of
targets in large gene families. Identified specific chemistries are used as
critical tools to help elucidate the therapeutic potential of these targets.
Equally important, once functionally relevant and drug-like chemistries are
discovered for a given target, efficient lead optimization efforts may be
rapidly initiated.
ACADIA's chemical genomics efforts have focused on two gene families that
are particularly rich in drug targets, the GPCRs and nuclear receptors.
Together, these two important gene families are believed to be the targets of
more than half of the known drugs. ACADIA has established functional assays
for more than 250 targets out of the approximately 500 GPCRs and nuclear
receptors within its chemical-genomics platform. To date, ACADIA has applied
its chemical-genomics approach to over 100 of these targets, and has
successfully identified novel small molecule chemistries for more than
60 targets.
"It is very exciting to compare the chemistries for such a diversity of
targets," said Mark R. Brann, Ph.D., ACADIA's President and Chief Scientific
Officer. "This approach has provided ACADIA with a wealth of opportunities
for drug discovery programs and has already led to several drug candidates
rapidly approaching the clinic. In addition, we have identified the first
ligands for several unexploited targets that provide us with new and exciting
program opportunities. Two particularly interesting examples are small
molecule agonists for HNF4-alpha and PAR2. HNF4-alpha is an orphan nuclear
receptor that when mutated causes MODY, a form of diabetes mellitus. While
HNF4-alpha is an exquisitely well-validated target, the pharmaceutical
industry has not reported suitable small molecule chemistries for this target.
PAR2 is a GPCR that is activated by the protease trypsin. Many lines of
evidence point to a role of this receptor in inflammatory disease and
neuropathic pain. These exciting discoveries position ACADIA to launch the
first small molecule drug discovery efforts aiming at innovative therapies
that exploit HNF4-alpha and PAR2 modulation."
ACADIA has used its chemical-genomics platform to generate a broad drug
discovery pipeline that addresses large unmet medical needs and major
commercial markets, including psychosis. "Our inverse agonist for the 5HT2A
receptor, ACP-103, is scheduled to enter clinical trials later this year,"
said Robert E. Davis, Ph.D., ACADIA's Executive Vice President of Drug
Discovery and Development. "In this program, we used our chemical-genomics
platform to rapidly identify compounds with the desired combination of
potency, specificity and efficacy for use as antipsychotics. In our
muscarinic m1 psychosis program, our platform enabled the discovery of highly
specific chemistries that interact with a unique 'ectopic' binding site on the
m1 receptor. This discovery led to a program now in late-stage preclinical
testing, which positions ACADIA to exploit the therapeutic opportunities
afforded by the first truly selective m1 agonist."
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.
For further information please contact Mark R. Brann, Ph.D., President and
CSO, or Douglas E. Richards, VP of Business Development, of ACADIA
Pharmaceuticals, +1-858-558-2871. |
