ACADIA Expands Pain Portfolio to Include New GPCR Targets
Discovery of First Small Molecule Agonists for NPFF and MrG Receptors
SAN DIEGO, CA, December 10, 2002 - ACADIA Pharmaceuticals announced
today the discovery of the first small molecule chemistries that activate two
important G-protein coupled receptor (GPCR) targets, the NPFF and the MrG receptors.
Small molecule drugs acting on these recently discovered targets represent a
potential breakthrough in the treatment of pain. ACADIA's novel lead chemistries
broaden the Company's therapeutic pain portfolio, which also includes ACP-102,
a GPCR agonist that is scheduled to enter clinical development shortly for the
treatment of neuropathic pain in cancer patients, and preclinical compounds
that target a specific subtype of the muscarinic receptors.
NPFF and MrG receptors are members of the family of gene products referred
to as GPCRs. This family represents the targets of a diversity of blockbuster
drugs and genomic efforts have shown the existence of more than 400 pharmaceutically
relevant GPCRs. Most of these GPCRs have no known hormones or chemistries that
activate them, and are referred to as "orphan" receptors. NPFF receptors
are prominently expressed in the spinal cord where they mediate the analgesic
responses of the peptide NPFF. Recently, NPFF was found to activate one of the
orphan receptors present in the spinal cord. The MrG receptors are orphan GPCRs
that are exclusively expressed by the neurons in the dorsal root ganglia that
transmit pain signals to the central nervous system.
"To our knowledge, we have discovered the first small molecule chemistries
that activate these targets," said Mark R. Brann, Ph.D., ACADIA's President
and Chief Scientific Officer. "The chemistries are potent, selective and
drug-like. In the case of the MrGs we have a range of chemistries that differentiate
among the subtypes. It is very exciting to launch drug discovery programs in
completely new areas where the biology is so compelling." These chemistries
were initially found through ACADIA's chemical-genomics approach, where ACADIA
is systematically screening members of the GPCR gene family in the search for
novel 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 pain
therapeutics," said Robert E. Davis, Ph.D., ACADIA's Executive Vice President
of Drug Discovery and Development. "We have two other pain programs: ACP-102
that also targets a GPCR and our advanced preclinical program that exploits
muscarinic receptors. We have the necessary preclinical models and development
capabilities to rapidly push these new opportunities forward."
ACADIA Pharmaceuticals is a drug discovery and development company that efficiently
discovers small molecule drug candidates using its proprietary chemical-genomics
platform. ACADIA has successfully applied its platform to generate a broad discovery
pipeline that includes advanced programs directed at major diseases, including
Parkinson's disease, 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.
Douglas E. Richards, VP of Business Development