Positive results of enx-101 clinical 1b study published by English topics

Ready to start the second phase ENACT Focal epilepsy test
• ENX-101 It shows good safety and pharmacokinetic characteristics in healthy subjects
• Take it orally once a day ENX-101 The was well tolerated , Dose titration is not required
• Transformed biomarker data show ,ENX-101 Its targeting effect is consistent with its antiepileptic activity
• Engrail Plan to start the second phase ENACT Epilepsy test

Engrail Therapeutics（Engrail）（ abbreviation “ company ”） It is an M & a focusing on transformational therapy 、 Research, development and commercialization of neuroscience companies . Company announcement ENX-101 Subtype selectivity GABA-A Receptor positive allosteric modulator （PAM） Clinical 1b The experiment yielded positive results , Relevant data have been published on 2022 year 6 month 6 Held in Santa Clara, California, USA 2022 Epilepsy R & D project conference （2022 Epilepsy Pipeline Conference） Announced on . Based on these research results and the company's recent contact with the U.S. Food and Drug Administration on adjusting the phase II development project ,Engrail Plan to start ENACT International multicenter phase II clinical trial , To evaluate ENX-101 The efficacy and safety of this drug in patients with focal epilepsy .

Engrail Therapeutics Chief scientific officer Kimberly Vanover Doctor said ：“ We are pleased to announce that different doses of ENX-101 Excellent safety and tolerability in healthy subjects . Transformed biomarker data also clearly demonstrate ENX-101 Targeting effect of , It is expected to bring positive clinical benefits to patients with epilepsy and other central nervous system diseases .”

Take orally once a day for ten days ENX-101 It is safe and well tolerated for healthy subjects , About the representation of life 、 electrocardiogram 、 There were no clinically significant dose-related changes in physical examination and clinical laboratory values . Adverse events during treatment are generally mild and transient , No serious or serious adverse events were reported . Most common during treatment and administration ENX-101 The related adverse event was mild transient lethargy , It mainly occurs in the first few days of taking medicine . Studies have shown that , forecast ENX-101 The exposed dose half-life is about 20 Hours .

ENX-101 Show activity in multiple pharmacodynamic biomarkers , Confirmed its targeting effect . especially ,ENX-101 Reduced peak saccade speed , And central action type GABA-A PAM Pharmacologically consistent , And improved the quantitative EEG record beta energy . Repeated application ENX-101 To vigilance 、 The effect of mental activity function or sustained concentration is extremely slight or even zero .ENX-101 Nor did it show a similar sedative effect , Quantitative EEG delta Energy does not increase but decreases . Besides , There is no evidence of repeated application ENX-101 It will develop rapid resistance to functional targeting , Or have tolerance to central nervous system inhibition . To sum up , Relevant research data and GABA Mediated pharmacodynamic properties are consistent , It is different from sedative hypnotics and other non selective drugs GABA-A PAMs.

Professor of Neurology, langney health comprehensive epilepsy center, New York University Jacqueline French The doctor said ：“ENX-101 The research data so far are very encouraging . Epilepsy, a stubborn disease, needs better treatment options , expect ENX-101 It will help patients with intractable epilepsy .”

Engrail CEO and President Vikram Sudarsan The doctor added ：“ except ENX-101 clinical 1b The positive results of the study are very encouraging , The company will be more Many other important achievements are expected .Engrail On 2019 It was founded in with the goal of becoming a leading neuroscience company . Our excellent team is experienced , A unique and solid development portfolio has been established , Its six projects have their own characteristics , Two of them also quickly entered the second stage of research . The whole development project portfolio is based on rigorous business development strategy and internal drug research and development work , We are trying our best to push forward the progress of all projects .”

About ENX-101-004 1b test
ENX-101-004 It is a randomized study of healthy subjects 、 Placebo control 、 Multi dose incremental test . The subjects took orally once every morning ENX-101 Or a placebo , Last ten days . Five groups of subjects （N=9; The proportion of each group receiving active drug and placebo is 6：3） Of ENX-101 The dosages are 5、10、15、25 And 50 mg . The main purpose of the study was to evaluate ENX-101 Safety and tolerability after repeated administration ; Secondary objectives include assessing ENX-101 On ECG （ECG） Parameters 、 Pharmacokinetics （PK） Parameters and a series of pharmacodynamic biomarkers （ Such as saccade 、 Quantitative EEG （qEEG） Parameters 、 Visual analogue scale and cognitive performance ） Influence .

Screening period （ The first -28 Tianzhidi -3 God ） after , Healthy subjects eligible for inclusion were enrolled in the baseline period （ The first -2 Tianzhidi -1 God ） Admitted to the clinical research center . The study treatment was carried out in 1 Tianzhidi 10 Days go on , The subjects were followed up for three days after the treatment was stopped , And in the first place 13 Days after discharge . Study at baseline 、 The first 2 God and 9 Days to collect a lot of biomarker information , Safety and tolerability were assessed daily .

About ENX-101
Targeting γ- Aminobutyric acid A type （GABA-A） Receptors are well proven pharmacological methods , For the treatment of epilepsy 、 anxious 、 Pain and other central diseases . However , Traditional non selective GABA-A Receptor modulators （ Such as benzodiazepine 䓬 Drugs ） A number of disadvantages of the limited long-term use , Mainly because it contains GABA-A α1 The channel of subunits .ENX-101 It is a precise target in research GABA-A Receptor positive allosteric modulator , Can be enhanced to contain α2、α3 And α5 The receptor of subunit is blocked by nerve conduction α1. This feature is believed to contribute to antiepileptic efficacy , With good safety , And will α1- Mediated GABA To minimize the adverse effects related to neurotransmission . Take it orally once a day ENX-101 Good tolerability in clinical trials , Dose titration is not required .

About Engrail Therapeutics
Engrail Founded on 2019 year , We are committed to opening up a new direction for reducing the pressure of nervous system diseases on patients and society . We combine biological insights with viable clinical solutions , Build and promote a variety of transformational drug combinations . We use rigorous scientific methods to identify the most promising treatments , Use flexible trading models to promote assets whose mechanisms have been proven , And effectively transform it into commercial products .Engrail Nanfeng life technology provides long-term capital commitment .