Mundipharma Medical Company Limited and its independent associated company, Purdue Pharma LP, announced that, following completion of Phase II studies, they have exercised their option and taken over full responsibility from Laboratorios ESTEVE, SAU. (ESTEVE) for the clinical, regulatory and commercial development of a potential first-in-class sigma-1 antagonist (S1A or MR309/E-52862).
Mundipharma and ESTEVE recognise that the problem of pain is not solved and are committed to developing new treatments to help patients better manage their pain. The addition of this asset to the Mundipharma pain pipeline continues the growth of the global pain franchise, an area of deep heritage and experience for the Mundipharma network of independent associated companies worldwide.
MR309/E-52862 is a potent and highly selective sigma-1 antagonist that may provide a new way to approach the management of neuropathic pain, one of the most challenging pain conditions to manage.
Studies suggest that the novel mechanism of action of MR309/E-52862 will be complementary to those of other drugs used in pain management and may therefore support combination usage with other analgesic compounds. Furthermore, it offers the potential for improvement over current therapeutic options, as many currently available treatments for pain are associated with troublesome side effects, limited efficacy, frequent dosing and/or titration.
MR309/E-52862 binds to sigma-1 in the brain and central nervous system. To date, activity has been demonstrated in vitro and in vivo in multiple models of neuropathic pain, including nerve injury and diabetic neuropathy. These studies have also proven that there is a direct relationship between dose, target occupancy of MR309/E-52862 in the brain and pharmacological activity.1
In the Phase I programme, in which human subjects were administered MR309/E-52862, good safety, tolerability, pharmacodynamic and pharmacokinetic profiles were observed at all doses tested.2,3
Phase II clinical studies on patients treated with MR309/E-52862 in peripheral neuropathy of different aetiologies (including from diabetic and post-surgical origins) as well as in moderate to severe acute post-operative pain have been conducted and the results are pending publication. Mundipharma will now take the programme forward into additional clinical studies to support the ongoing development in multiple models of neuropathy and future registration and commercialisation.
Antony Mattessich, Managing Director, Mundipharma International Limited commented on the partnership. “We’re very excited about the opportunity to realise the potential of MR309/E-52862 to help patients and healthcare professionals manage neuropathic pain in an area of high unmet need. MR309/E-52862 will form a key part of our growing pain pipeline, and will add to our heritage and leadership in the area. We’re also thrilled to expand our partnership with ESTEVE. This strategic collaboration leverages our companies’ individual strengths. Our ability to bring products through the clinical and regulatory process and to successfully commercialise them complements ESTEVE’s focus on discovering novel approaches to the treatment of pain in the laboratory. Mundipharma, Purdue and ESTEVE are equally committed to driving innovation in pain management, so our ongoing collaboration is a natural fit.”
Albert Esteve, Chief Executive Officer, ESTEVE, said: “This partnership with Mundipharma will, we hope, allow patients to have access to a new class of treatment to manage pain. Together, we will foster the development of a first-in-class new molecular entity targeting a novel mechanism of action for pain relief. The alliance with Mundipharma and Purdue strengthens the validation of our innovative first-in-class NME R&D and our mission statement, which is to advance science by establishing novel R&D collaborations and to solve unmet medical needs of diseases with significant social impact.”
- Romero L et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol 2012;166(8):2289–306.
- 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;75(1):103–17.
- Täubel J et al. Single doses up to 800 mg of E-52862 do not prolong the QTc interval–A retrospective validation by pharmacokinetic-pharmacodynamic modelling of electrocardiography data utilising the effects of a meal on QTc to demonstrate ECG assay sensitivity. PLoS One 2015;10(8):e0136369.