Neurolixis Announces Scientific Publication Demonstrating Rapid and Long-Lasting Antidepressant Activity of NLX-101 in a Robust Rodent Model

DANA POINT, Calif. - July 22, 2019 - PRLog -- Neurolixis, Inc. announced the publication of scientific data demonstrating rapid and long-lasting antidepressant activity of the Company's 'biased agonist' drug candidate, NLX-101 in a robust rodent model of depression. The study, published in the Journal of Psychopharmacology, showed that NLX-101 produced very rapid (i.e. within 1 day) and complete reversal of depressive-like behavior in rats subjected to chronic mild stress. Furthermore, the antidepressant-like activity of NLX-101 was maintained for several weeks after cessation of drug administration, suggesting a long-lasting remodeling of neuronal networks controlling some aspects of mood. NLX-101 also rescued cognitive function that had been impaired by  chronic mild stress.

The experiments were conducted in the laboratory of Prof. Mariusz Papp (Institute of Pharmacology, Polish Academy of Sciences, Krakow, Poland), a leading researcher in the field of antidepressant drugs. Prof. Papp commented: "The chronic mild stress model is highly validated and predictive of human antidepressant efficacy. Our laboratory has tested many antidepressant drugs, including reuptake inhibitors and ketamine, using the same conditions as those we used for NLX-101. However, none of the other drugs exhibited such rapid effects as NLX-101."

Adrian Newman-Tancredi, PhD, DSc, Chief Scientific Officer of Neurolixis, commented: "We are excited about the remarkable activity of NLX-101 in this highly regarded model of depression. There is a great need for antidepressant drugs that are efficacious and well-tolerated. These striking results support our efforts to develop novel, rapid-acting, antidepressants based on the NLX-101 scaffold. If the rodent data translate to the clinic, these biased agonist compounds could significantly alleviate depression symptoms and other mood deficits, thus improving many patients' quality of life."

Details of the scientific publication
Cortical 5-hydroxytryptamine 1A receptor biased agonist, NLX-101, displays rapid-acting antidepressant-like properties in the rat chronic mild stress model.
Depoortère R, Papp M, Gruca P, Lason-Tyburkiewicz M, Niemczyk M, Varney MA, Newman-Tancredi A. J Psychopharmacol. 2019. doi: 10.1177/0269881119860666. PMID:  31290370

About Novel 5-HT_1A Receptor Biased Agonists
In collaboration with a team led by Dr. Marcin Kołaczkowski (Jagiellonian University, Krakow, Poland), Neurolixis is developing a series of potent and highly active 5-HT_1A receptor biased agonists that are analogs of NLX-101 and exhibit promising in vitro selectivity, potent in vivo antidepressant-like activity and favorable developability profiles. NLX-101 is a first-in-kind selective, efficacious 'biased agonist' that preferentially targets serotonin 5-HT_1A receptors located in cortical regions of the brain which control mood and cognition. NLX‑101 has undergone initial testing in human volunteers and has an 'open IND' from the FDA, so it is ready for Phase 1 clinical trials. The novel analogs have been patented (WO/2017/220799) and are undergoing lead-to-candidate selection.

About Major Depression
Major depression is a leading cause of disability with over 16 million patients in the USA. Most existing antidepressants act by inhibition of neurotransmitter reuptake but require many weeks of treatment before they are effective and only about half of patients respond satisfactorily. The anesthetic drug, ketamine, exhibits rapid-acting antidepressant (RAAD) activity in treatment-resistant patients but it elicits marked side-effects which limit its use.  Recent findings indicate that ketamine indirectly activates 5-HT_1A receptors in cortical brain regions, suggesting that their direct activation may elicit promising RAAD activity with improved safety and tolerability.

About Neurolixis, Inc.
Neurolixis, located in Dana Point, California, is a privately held biotechnology company developing therapies for disorders of the central nervous system. Its biased agonist drug discovery program targets major depression, NLX-101 is Phase 1-ready as a treatment for Rett syndrome (an orphan indication), and NLX-112 is Phase 2-ready as a treatment for L-DOPA-induced dyskinesia in Parkinsonian patients. Further information is available at http://www.neurolixis.com.

Forward Looking Statement
Except for the historical information contained herein, the matters discussed in this press release are forward-looking statements that involve risks and uncertainties, including: our dependence on third parties for the development, regulatory approval and successful commercialization of our products, the inherent risk of failure in developing product candidates based on new technologies, risks associated with the costs of clinical development efforts, as well as other risks. Actual results may differ materially from those projected. These forward-looking statements represent our judgment as of the date of the release. Neurolixis disclaims any intent or obligation to update these forward-looking statements.