R-Tech Ueno, Ltd. has announced plans to conduct collaborative research with Autonomous University of Barcelona (UAB) and Vall d’Hebron Institute of Research (VHIR), in Catalonia (Spain) to develop a novel VAP-1 inhibitor (Development code: RTU-009) for treatment of cerebral infarction.

RTU-009 is a novel VAP-1 inhibitor, having an anti-inflammatory and neuroprotective effect. It is confirmed that RTU-009 has a neuroprotective effect similar to Edaravone (Radicut), the brain protective agent, and a cerebral dysfunction improving effect when applied in combination with t-PA treatment in animal stroke models. It is currently undergoing non-clinical studies to proceed to Phase I clinical trials. Though an oral VAP-1 inhibitor named RTU-1096 is under development, RTU-009 is the novel VAP-1 inhibitor that has been developed as an injection agent targeting for treatment of acute cerebral infarction.

To explore the possibility of the clinical application of RTU-009 for treating cerebral infarction as a POC (Proof of Concept) trials (Early phase II clinical trials), we started collaborative research using stroke animal models with the group led by Professor Unzeta of the Institute of Neuroscience, UAB, and the group led by Dr. Montaner, MD, of the Neurovascular Research Laboratory of Vall d’Hebron Institute of Research, the research centre of the UAB-affiliated Vall d'Hebron University Hospital, who are active in the front line of clinical as well as research activity.

Going forward, we will proceed with the development of RTU-009 as a combination with t-PA treatment for acute cerebral infarction as the top priority target. These initiatives, including early clinical trials, will be conducted in collaboration with academia.

Yukihiko Mashima, president of the company, has said: "The number of stroke patients is estimated to reach 3 million people in 2020, and once a stroke has occurred, patients are likely to suffer from related aftereffects. Considering the policy to extend a healthy life, as stated by the Ministry of Health, Labour and Welfare in Japan, as well as from the perspective of the medical economy, it is necessary to proceed with the strategy to suppress the increasing population of patients suffering from the aftereffects of stroke.

For the acute stage of cerebral infarction, thrombolytic treatment using t-PA is the first-line therapy; however, t-PA can only be used for patients within 4.5 hours from the onset of stroke, considering the risk of brain haemorrhage. Therefore, it is extremely important to develop a new treatment method that reduces the risk of brain haemorrhage and enlarges the range of target patients. According to some reports, the recovery rate, representing the rate of patients who recover to the level of self-reliance, with t-PA treatment is 40-50% in Japan. Further enhancement of the recovery rate and expansion of the 4.5-hour time window for treatment are strongly desired in clinical practice, and we may achieve such goals by utilizing RTU-009 as combination with t-PA treatment. In addition, it was recently reported that removing the thrombus in treatable patients within 6 hours of stroke onset via endovascular treatment (mechanical thrombus collection therapy or endovascular thrombectomy) improves treatment results as compared with conventional treatments. Based on this report, we would like to also explore a new treatment utilizing RTU-009, which has an anti-inflammatory effect, in combination with endovascular treatment.

Professor Unzeta is the leading researcher for the VAP-1 study, and she is targeting the diseases of cerebral infarction and Alzheimer disease now. Dr. Montaner plays a central role in clinical trials related to stroke in Spain. He conducted collaboration studies with Professor Unzeta on acute cerebral infarction treatment utilizing VAP-1 inhibitors in the animal models. By collaborative research with Professor Unzeta and Dr. Montaner this time, R-Tech Ueno attempts to rapidly proceed with clinical trials of RTU-009. Vall d'Hebron University Hospital had established systems to conduct Phase I trials and POC trials under the direction of Dr. Montaner. By taking advantage of this framework, we plan to promote the development of RTU-009 as a new treatment to be used in combination with t-PA through collaboration with academia."