ESTEVE Announces the Publication of Comprehensive Phase I Data for a Novel Oral, First-in-class New Chemical Entity (NCE),E-52862, a Sigma-1 Receptor Antagonist (S1RA) Being Developed for Pain
BARCELONA, Spain, September 4, 2012/PRNewswire/ --
- E-52862 is a potent, highly selective NCE with
a novel mechanism of action
(MOA; Sigma 1 Receptor (S1R)
antagonism) currently being evaluated for the treatment
of pain
- Key data are outlined from three Phase I
studies involving 175 male and female
human subjects
- These studies demonstrate a favourable safety,
tolerability, pharmacokinetic
and pharmacodynamic profile for
E-52862
- Phase II clinical trials evaluating E-52862
are ongoing
ESTEVE announces the recent publication of data from the Phase I
clinical trial programme of a novel, highly potent and selective,
once-daily, S1RA E-52862, developed by the ESTEVE R&D team, in
the British Journal of Clinical Pharmacology[1].
(Logo: http://photos.prnewswire.com/prnh/20120904/554843
)
Mariano Sust, M.D., corresponding author, stated that "E-52862 represents a NCE with a novel, unprecedented mechanism of action for pain of different aetiologies. We are very encouraged by these results and look forward to future findings from the E-52862 clinical trial programme in due course."
To fully validate the safety and tolerability of E-52862, ESTEVE
performed a rigorous phase I programme. This publication reports
results from three, Phase I studies involving 175 human subjects.
E-52862 demonstrated a favourable safety and tolerability profile
across a robust panel of assessments including adverse event
recording following questioning and spontaneous reporting; physical
examinations; vital signs measurements; laboratory safety tests
(haematology, blood coagulation, biochemistry, urinalysis);
multiple psychometric tests; computerized cognitive evaluations
(including assessment of executive function, working memory and
learning, reaction time and psychomotor functions); and thorough
cardiac monitoring (telemetry, triplicate 12-lead ECGs, 24-hour
Holter ECGs). Pharmacokinetic assessments were performed in each
study and results demonstrate a favourable pharmacokinetic and
pharmacodynamic profile, supporting oral, once-daily administration
of E-52862.
The E-52862 Phase I programme is now complete and included over 300
human subjects (more than 250 received E-52862). Results from the
overall programme show favourable safety, tolerability,
pharmacodynamic and pharmacokinetic profiles at all doses of
E-52862 tested.
Today, the E-52862 clinical programme focuses on pain management -
highlighting both neuropathic pain and the potentiation of opioid
analgesia. The Phase II clinical trial programme for E-52862 began
early in 2012. The clinical project leader for E-52862, Roser
Vives, M.D. commented that "Because of the MOA and data available
to date, we are evaluating E-52862 in four different types of
neuropathic pain and for treatment of pain in patients receiving
opioids (for the enhancement of the analgesic effect and better
tolerability). E-52862 also has potential applications for other
neurological and psychiatric indications".
E-52862, whose MOA is both novel and complementary to that of other
analgesic compounds, could provide a much-needed addition to future
pain management choices with, perhaps, the option to be used as
monotherapy, as well as in combination with other pain relief
compounds, depending on the type of patient and clinical
indication.
About ESTEVE
ESTEVE is a leading pharmaceutical chemical group based on
Barcelona (Spain) with significant international presence. Since it
was founded in 1929, ESTEVE has been firmly committed to excellence
in healthcare, dedicating efforts to innovative R&D of new
medicines for unmet medical needs and focusing on high science and
evidence-based research. ESTEVE has a strong partnership approach
to drug discovery, development and commercialisation. The company
works both independently and in collaboration to bring new,
differentiated best-in-class treatments to patients who need them.
The company currently has a team of about 2800 professionals, and
has subsidiaries and production facilities in several European
countries, USA, China and Mexico.
About E-52862 and Pain R&D at ESTEVE
ESTEVE's dedicated in-house R&D team is focused on the
development of novel pain medications, an area of high unmet
medical need. Considerable progress in the knowledge of the biology
and pharmacology of the S1R (a unique protein) during recent years
has re-energised research into the potential benefits of S1R
ligands in a range of neurological and psychiatric conditions.
New data has addressed key questions on modulation, MOA and
pathophysiology of the S1R. The proprietary knockout mouse
demonstrated a direct role of the S1R in sensitisation phenomena
associated with neuropathic pain mechanisms and behaviours. E-52862
exerts robust, dose-dependent analgesic activity in multiple
preclinical neuropathic pain models and enhances opioid analgesia.
E-52862 could have potential applications for other neurological
and psychiatric indications. Besides information reported here, an
extensive preclinical regulatory safety package is available for
E-52862 (including 13-week repeat dose toxicity studies in various
animal species). E-52862 also has robust intellectual property
protection.
ESTEVE's portfolio in pain also includes a technology
platform-derived new co-crystal entity (E-58425) developed by the
in-house R&D team. E-58425 has completed Phase I, with Phase II
currently ongoing. E-58425 is being developed for moderate to
severe acute and chronic pain.
Reference
[1]Abadias, M. et al. Safety, Tolerability and Pharmacokinetics of
Single and Multiple Doses of a Novel Sigma-1 Receptor Antagonist in
Three Randomized Phase I Studies. Br J Clin Pharmacol 2012 [Epub
ahead of print]. DOI: 10.1111/j.1365-2125.2012.04333.x
For more information and enquiries into partnership opportunities,
please contact:
Mark Mayhew, PhD, Head of ESTEVE R&D Strategic Partnering, Tel.
+34-93-446-6000, mmayhew@esteve.es
For corporate communications/media enquiries, please contact:
Ma. Angels Valls, Head of ESTEVE Corporate Communications, Tel.
+34-93-446-6000, avalls@esteve.es
Visit our new R&D website: http://www.esteve.com/research-development
Follow us on Twitter: @ESTEVE_news
Photo: http://photos.prnewswire.com/prnh/20120904/554843
Source: ESTEVE
Posted: September 2012
