Data from ESTEVE’s S1RA E-52862 Phase I trial programme on pain

Sep 4 2012

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.

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.