Cara's most advanced drug candidate in
development, CR665, is a highly specific kappa opioid agonist with
physical properties that ensure an unprecedented level of selectivity
for kappa receptors located on peripheral nerves. Therapeutic indications
for “peripherally-restricted” kappa
agonists include,
but are not restricted to, post-operative pain and ileus associated
with abdominal surgery, pancreatitis pain, dysmenorrhea, labor pain,
and irritable bowel syndrome. In addition to their utility as analgesics,
kappa agonists have been recognized to possess unique anti-inflammatory
actions which may be useful in the treatment of diseases such as rheumatoid
arthritis. CR665 has completed clinical Phase 1a studies and is moving
into Phase 2a studies and is currently undergoing proof-of-concept Phase 2a trials.
Cara is also developing molecules that selectively
modulate peripheral
CB2 receptors. CB2 receptors are found predominantly in peripheral
tissues, particularly immune cells such as leukocytes
and mast cells, which have been shown to be involved
in pain and inflammatory responses.
This approach follows the same logic outlined for
the development of peripherally acting kappa opioids,
which is to develop novel pain medications
without the side effects associated with brain receptor
activation.Peripheral CB2 receptor modulators will be developed as a novel
therapeutic approach for neuropathic pain, a condition
currently without consistently
effective therapies. Cara's lead CB2 compounds are
currently in preclinical development.
Cara's screening technology, referred to as GPCR DimerScreen™ ,
is designed to specifically and selectively identify molecules interacting
with GPCR dimers and thus allows for the discovery of compounds with
new pharmacological properties at identified dimeric drug targets.
Cara will focus on the identification of new chemical entities to modulate
dimeric receptor drug targets relevant for the treatment of pain and
inflammation. This novel approach provides a competitive advantage
in drug discovery to Cara since it offers opportunities for “first-in-class” therapeutics
that could dramatically alter standard treatment of these conditions.
|