ACADIA Expands Pain Portfolio to Include New GPCR Targets
Discovery of First Small Molecule Agonists for NPFF and MrG Receptors
2002-12-10 08:04 (New York)
SAN DIEGO, Calif., Dec. 10 /PRNewswire/ -- 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. |
