공시 • Nov 20
Eupraxia Pharmaceuticals Inc. Diffusphere Technology Demonstrates Targeted Drug Release While Minimizing Systemic Exposure for A Period of More Than Six Months
Eupraxia Pharmaceuticals Inc. unveiled new pharmacokinetic data from its Phase 2a Eosinophilic Esophagitis program. Management believes these data underscore the unique capabilities of Eupraxia's proprietary DiffuSphere™ platform technology, which aims to provide precise, localized, safe, and effective long-lasting drug delivery. Most conventional drugs release in a pattern characterized by steep peaks and rapid declines in drug concentration, where peaks often lead to negative side effects, and troughs result in reduced efficacy. In contrast, DiffuSphere is a unique microsphere that is designed to enable precise drug release into target tissues with a flat, stable, and long-lasting profile, minimizing potential adverse events associated with high-dose systemic delivery. What sets DiffuSphere™ apart is its composition: a pure drug crystal encased in a microns-thick polymer shell. Eupraxia's proprietary technology uses this polymer to precisely control a drug's release, ensuring high drug concentrations in the target tissues while minimizing exposure to the rest of the body. This innovative approach has been observed in Eupraxia's clinical programs, demonstrating precision, tolerability, and extended duration of delivering fluticasone propionate ("FP") directly to the intended tissues for EoE and knee osteoarthritis ("OA") patients. DiffuSphere, when injected into the esophageal wall (submucosa), shows a treatment duration exceeding six months from a single injection, with predictable dose control. In Cohort 1 (4 mg FP), a steady level of 1.5 pg/ml was maintained for at least six months. In Cohort 5 (48 mg FP), 10pg/ml was observed at three months. With this steady, localized, and long-lasting delivery, key EoE disease measures, including patient symptoms, esophageal tissue health, and eosinophil counts, improved. This impact of the DiffuSphere technology was clearly demonstrated in a non-clinical study in pigs comparing local and systemic levels of FP after intraesophageal injection of EP-104GI versus oral gavage. Presented at the American College of Gastroenterology meeting (poster), the study revealed that esophageal tissue levels of fluticasone were more than 1000 times higher in the EP-104GI group compared to the oral gavage group, even at distances of several centimeters from the injection sites. Moreover, despite significantly higher local concentrations, systemic levels of fluticasone in the plasma were lower in the EP-104IAR group than in the oral gavage group. This underscores the targeted and precise delivery capabilities of the DiffuSphere technology. DiffuSphere is the technology behind Eupraxia's EP-104IAR for treating OA. In Eupraxia's Phase 2b clinical study, EP-104IAR was well tolerated and showed significantly durable efficacy over placebo. The trial results were recently published in TheLancet, reinforcing the preclinical work previously published in Cartilage. The Phase 2b data showed that EP-104IAR effectively controlled patients' pain for up to 22 weeks (as measured by OARSI Strict Responders) and was well-tolerated. This includes no disruption to blood glucose metabolism (a key factor for diabetics, who comprise almost 40% of the OA population) or adrenal function, which have been reported with other steroid formulations used in this indication. Eupraxia has successfully applied DiffuSphere™ across multiple anatomic locations and drug classes. In preclinical studies, DiffuSphere™ has demonstrated its precise, steady, and tunable delivery traits in intraarticular, intraesophageal, intravitreal, epidural, peritoneal, and subcutaneous applications. Additionally, Eupraxia has demonstrated DiffuSphere's™ capability with local anesthetics such as ropivacaine and various anti-infective agents. The new data in EOE patients further supports DiffuSphere's ability to deliver drugs with local precision: stable drug delivery without peaks and troughs, and a customizable duration to fit the clinical indication. This reinforces Eupraxia's confidence in the platform's broad potential. Eupraxia's OA product candidate, EP-104IAR, is designed to meet the significant unmet medical need and market demand for long-lasting disease relief in multiple indications, benefitting from highly localized and longer delivery of corticosteroids. The lead indication is for pain relief in knee OA. The U.S. Centers for Disease Control and Prevention estimates knee OA affects more than 30 million people in the U.S. alone. This includes 14 million that suffer from knee pain or some form of disability. Knee OA is also associated with depression and loss of sleep, which can significantly affect quality of life. With EP-104IAR, Eupraxia hopes to change the way knee OA pain is treated. The Company believes current therapies are challenged by poor safety, inadequate efficacy and/or limited duration of activity. Corticosteroids are one of only two drug classes strongly recommended by the American College of Rheumatology and the Arthritis Foundation for treating knee OA pain. Currently approved corticosteroids are very effective at reducing pain for a short duration late in the disease but can expose the body to unwanted local and systemic side effects. EP-104IAR is designed to prolong the duration of pain relief with fewer adverse events. It encapsulates a highly potent corticosteroid (fluticasone propionate) within a microns-thin polymer membrane, part of Eupraxia's patented technology platform. Injected into the knee, EP-104IAR is designed to diffuse the corticosteroid slowly into the knee joint providing local therapeutic concentrations for up to six months. This has the potential dual advantage of providing longer duration of pain relief with fewer systemic adverse events. A robust safety and tolerability profile would also benefit the estimated 70% of knee OA patients that experience pain in both knees by allowing simultaneous treatment of both affected joints. EP-104IAR has also been designed to incorporate additional advantages, such as physician convenience, targeting a long shelf life, no refrigeration and easy integration into existing delivery techniques.
