M5 receptor x M4 receptor

SAN DIEGO, May 9, 2024 /PRNewswire/ -- Neurocrine Biosciences, Inc. (Nasdaq: NBIX) today announced the initiation of its Phase 1 first-in-human clinical study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of investigational compound NBI-1076986 in healthy adult participants. NBI-1076986 is an investigational, oral, M4 subtype-selective muscarinic acetylcholine receptor antagonist for the potential treatment of movement disorders that was discovered and developed by Neurocrine Biosciences. "This compound is an important part of our muscarinic portfolio, which enters the clinic as a potential treatment for movement disorders," said Eiry W. Roberts, M.D., Chief Medical Officer at Neurocrine Biosciences. "Selectively targeting M4 receptors could benefit a broad range of motor coordination disorders, including Parkinson's disease tremor and dystonia." About Muscarinic Pipeline and NBI-1076986 Muscarinic receptors are fundamental to activating signaling pathways in the brain. There are five muscarinic acetylcholine receptors involved in neurotransmission (M1–M5), with M4 receptors associated with motor coordination and certain central nervous system pathologies. M1 receptors play a role in higher cognitive processes such as learning and memory and are thought to be associated with the memory/cognitive side effects associated with non-selective antimuscarinic agents. Identified and developed by Neurocrine Biosciences, NBI-1076986 is an investigational, oral, M4 subtype-selective muscarinic acetylcholine receptor antagonist for the potential treatment of certain movement disorders, including Parkinson's disease tremor and dystonia. It is hypothesized that an M4 subtype-selective antagonist may impact regulation of motor symptoms and movements while minimizing off-target effects. Neurocrine Biosciences has a broad portfolio of programs that selectively target muscarinic receptors. In addition to NBI-1076986, the portfolio includes several small molecule M1, M1/M4 and M4 agonists that Neurocrine Biosciences acquired the rights to develop and commercialize from Nxera Pharma (formerly Sosei Heptares). About Neurocrine Biosciences Neurocrine Biosciences is a leading neuroscience-focused, biopharmaceutical company with a simple purpose: to relieve suffering for people with great needs, but few options. We are dedicated to discovering and developing life-changing treatments for patients with under-addressed neurological, neuroendocrine and neuropsychiatric disorders. The company's diverse portfolio includes FDA-approved treatments for tardive dyskinesia, chorea associated with Huntington's disease, endometriosis* and uterine fibroids*, as well as a robust pipeline including multiple compounds in mid- to late-phase clinical development across our core therapeutic areas. For three decades, we have applied our unique insight into neuroscience and the interconnections between brain and body systems to treat complex conditions. We relentlessly pursue medicines to ease the burden of debilitating diseases and disorders, because you deserve brave science. For more information, visit neurocrine.com, and follow the company on LinkedIn, X (formerly Twitter, and Facebook. (*in collaboration with AbbVie) The NEUROCRINE BIOSCIENCES Logo Lockup and YOU DESERVE BRAVE SCIENCE are registered trademarks of Neurocrine Biosciences, Inc. Forward-Looking Statements In addition to historical facts, this press release contains forward-looking statements that involve a number of risks and uncertainties. These statements include, but are not limited to, statements related to the potential benefits of NBI-1076986. Among the factors that could cause actual results to differ materially from those indicated in the forward-looking statements are: risks that clinical development activities may not be initiated or completed on time or at all, or may be delayed for regulatory, manufacturing, or other reasons, may not be successful or replicate previous clinical trial results, may fail to demonstrate that our product candidates are safe and effective, or may not be predictive of real-world results or of results in subsequent clinical trials; our future financial and operating performance; risks associated with our dependence on third parties for development, manufacturing, and commercialization activities for our products and product candidates, and our ability to manage these third parties; risks that the FDA or other regulatory authorities may make adverse decisions regarding our products or product candidates; risks that the potential benefits of the agreements with our collaboration partners may never be realized; risks that our products, and/or our product candidates may be precluded from commercialization by the proprietary or regulatory rights of third parties, or have unintended side effects, adverse reactions or incidents of misuse; risks associated with U.S. federal or state legislative or regulatory and/or policy efforts which may result in, among other things, an adverse impact on our revenues or potential revenue; risks associated with potential generic entrants for our products; and other risks described in the Company's periodic reports filed with the Securities and Exchange Commission, including without limitation the Company's quarterly report on Form 10-Q for the quarter ended March 31, 2024. Neurocrine Biosciences disclaims any obligation to update the statements contained in this press release after the date hereof other than required by law. Company Codes: NASDAQ-NMS:NBIX

Trelegy Ellipta is approved as a maintenance treatment for COPD and asthma in the US. Image Credit: MAXSHOT.PL / Shutterstock. Singapore’s Health Sciences Authority (HSA) has expanded the label of GlaxoSmithKline (GSK)’s Trelegy Ellipta (fluticasone furoate/umeclidinium/vilanterol) to include its use as a maintenance therapy for adults with asthma. The Singapore agency also approved a new dosage strength for the inhaled therapy in asthma. In 2019, HSA approved Trelegy Ellipta as a maintenance therapy for relieving moderate to severe exacerbations in patients with chronic obstructive pulmonary disease (COPD). Trelegy Ellipta is approved as a maintenance treatment for COPD in multiple regions including the US, Europe and China. However, the drug has also been approved for treating asthma in a few countries such as the US. Trelegy Ellipta pulled in £2.2bn ($2.8bn) in global sales for GSK in 2023, as per the company’s financials. The drug sales are expected to rise, with Trelegy Ellipta expected to generate approximately $3.8bn in global sales in 2027, according to a GlobalData analysis. GlobalData is the parent company of Pharmaceutical Technology . Last month, GSK announced plans to cap out-of-pocket costs for eligible patients at $35 per month for its COPD and asthma medications in light of the rising drug prices in the US. Trelegy Ellipta is one of the drugs included in GSK’s programme, which will be implemented across the country no later than 1 January 2025. See Also: UK MHRA approves Advanz Pharma antibiotic for complex infections Japan’s PMDA approves Partner’s inhaled Leukine for aPAP Another therapy looking to target both asthma and COPD populations is Amgen and AstraZeneca ’s Tezspire (tezepelumab-ekko). The monoclonal antibody has been approved for treating severe asthma in multiple countries including the US. The companies are evaluating the therapy in patients with moderate to severe COPD in a placebo-controlled Phase II trial (NCT04039113). Data from the trial is expected in H1 this year. Regeneron Pharmaceuticals and Sanofi are also seeking approval for their monoclonal antibody , Dupixent (dupilumab) as a maintenance therapy for COPD. The US Food and Drug Administration (FDA) has set a target action date of 27 June for an approval decision. Dupixent is approved for treating atopic dermatitis , asthma, chronic rhinosinusitis with nasal polyposis, eosinophilic esophagitis and prurigo nodularis.