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NBI-1117568
NBI-1117568 (former developmental code name HTL-0016878) is an investigational antipsychotic drug for schizophrenia that was out-licensed Nexera Pharma in to Neurocrine Biosciences, a United States-based pharmaceutical company. It is administered orally. Overview It is a selective muscarinic acetylcholine M4 receptor agonist that indirectly modulates dopamine as the basis for its putative improvement of schizophrenia. In April 2016, the compound was out-licensed to Allergan, an Irish pharmaceutical company. By September 2017, it had advanced to Phase I clinical trial for the indication of "neuropsychiatric symptoms associated with Alzheimer's disease and other dementias" However, in May 2020, Allergan was acquired by AbbVie, and due to AbbVie's pipeline business decisions, the license was returned to Nexceris in January 2021. In November 2021, the compound was newly out-licensed to Neurocrine Biosciences, a U.S. pharmaceutical company. It has been under development as a t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurocrine Biosciences
Neurocrine Biosciences, Inc. is an American biopharmaceutical company founded in 1992. It is headquartered in San Diego, California, and led by CEO Kyle Gano as of October 11, 2024. Neurocrine develops treatments for neurological and endocrine-related diseases and disorders. In 2017, the company's drug valbenazine (Ingrezza) was approved in the US to treat adults with tardive dyskinesia (TD). The company is also developing treatments that are in various stages of clinical research for Parkinson's disease, Tourette syndrome, and congenital adrenal hyperplasia and with a partner for endometriosis and uterine fibroids. History Neurocrine was founded in San Diego, California, in 1992. The company's academic founders were Wylie Vale of the Salk Institute for Biological Studies, and Lawrence Steinman of Stanford University. The company was backed by Avalon Ventures among others. In 1995, the company collaborated with Belgium-based Janssen Pharmaceutica N.V. to develop treatments ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Acetylcholine Receptor M4
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the ''CHRM4'' gene. Function M4 muscarinic receptors are coupled to Gi/o heterotrimeric proteins. They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the striatum. The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit functioning actively primarily in the hippocampus and cerebral cortex. Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M4 receptors in the striatum inhibit D1-induced locomotor stimulation in mice. M4 receptor-deficient mice exhibit increased locomotor simulation in response to D1 agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M4 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ML-007
ML-007 is a selective muscarinic acetylcholine M1 and M4 receptor agonist which is under development for the treatment of schizophrenia, psychotic disorders, and dyskinesias. It is being developed in combination with a peripherally selective muscarinic acetylcholine receptor antagonist (also known as ML-007/peripherally acting anticholinergic or ML-007/PAC). The drug is taken by mouth. As of January 2024, ML-007 is in phase 1 clinical trials for schizophrenia, psychotic disorders, and dyskinesias. It is under development by MapLight Therapeutics. The drug is a small molecule, but its chemical structure does not seem to have been disclosed. See also * Emraclidine Emraclidine (developmental code names CVL-231, PF-06852231) is an investigational antipsychotic for the treatment of both schizophrenia and Alzheimer's disease psychosis developed by Cerevel Therapeutics. On November 11, 2024, AbbVie announced ... * NBI-1117568 * NS-136 * Xanomeline/trospium Reference ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
M4 Receptor
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the ''CHRM4'' gene. Function M4 muscarinic receptors are coupled to Gi/o heterotrimeric proteins. They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the striatum. The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit functioning actively primarily in the hippocampus and cerebral cortex. Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M4 receptors in the striatum inhibit D1 receptor, D1-induced hyperlocomotion, locomotor stimulation in mice. M4 receptor-deficient mice exhibit increased locomotor simulation in response to dopamine agonist, D1 agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyrami ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Emraclidine
Emraclidine (developmental code names CVL-231, PF-06852231) is an investigational antipsychotic for the treatment of both schizophrenia and Alzheimer's disease psychosis developed by Cerevel Therapeutics. On November 11, 2024, AbbVie announced that phase 2 clinical trials did not show an improvement in Positive and Negative Syndrome Scale (PANSS) total scores from baseline when compared to the placebo group. Mechanism of action Emraclidine is a positive allosteric modulator that selectively targets the muscarinic acetylcholine receptor M4 subtype. The M4 receptor subtype is expressed in the striatum of the brain, which plays a key role in regulating acetylcholine and dopamine levels. An imbalance of these neurotransmitters has been linked to psychotic symptoms in schizophrenia. Unlike other muscarinic receptors Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NS-136
NS-136 is a selective muscarinic acetylcholine M4 receptor positive allosteric modulator which is under development for the treatment of schizophrenia and Alzheimer's disease. It has been found to possess pro-cognitive effects in rodents. The drug is under development by NeuShen Therapeutics. As of May 2024, it is in phase 1 clinical trials for schizophrenia and is in the preclinical stage of development for Alzheimer's disease. The drug is a small molecule, but its chemical structure does not seem to have been disclosed. See also * Emraclidine * NBI-1117568 * Xanomeline Xanomeline (developmental code name LY-246,708) is a small molecule muscarinic acetylcholine receptor agonist that was synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the tre ... References Drugs with undisclosed chemical structures Experimental drugs for Alzheimer's disease Experimental drugs developed for schizophrenia M4 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xanomeline/trospium
Xanomeline/trospium chloride, sold under the brand name Cobenfy, is a fixed-dose combination medication used for the treatment of schizophrenia. It contains xanomeline, a muscarinic agonist; and trospium chloride, a muscarinic antagonist. Xanomeline is a functionally preferring muscarinic M4 and M1 receptor agonist. Trospium chloride is a peripherally-acting non-selective muscarinic antagonist. The most common side effects of xanomeline/trospium chloride include nausea, indigestion, constipation, vomiting, hypertension, abdominal pain, diarrhea, tachycardia (increased heartbeat), dizziness, and gastroesophageal reflux disease. In September 2024, it was approved for medical use in the United States. It is the first antipsychotic drug approved by the US Food and Drug Administration (FDA) to treat schizophrenia that targets cholinergic receptors as opposed to dopamine receptors, which has long been the standard of care. The FDA considers it to be a first-in-class medication. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alzheimer's Disease
Alzheimer's disease (AD) is a neurodegenerative disease and the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in remembering recent events. As the disease advances, symptoms can include problems with language, disorientation (including easily getting lost), mood swings, loss of motivation, self-neglect, and behavioral issues. As a person's condition declines, they often withdraw from family and society. Gradually, bodily functions are lost, ultimately leading to death. Although the speed of progression can vary, the average life expectancy following diagnosis is three to twelve years. The causes of Alzheimer's disease remain poorly understood. There are many environmental and genetic risk factors associated with its development. The strongest genetic risk factor is from an allele of apolipoprotein E. Other risk factors include a history of head injury, clinical depression, and high blood pressure. The progression of the di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerevel Therapeutics
Cerevel Therapeutics Holdings, Inc. was an American biotechnology and pharmaceuticals company based in Cambridge, Massachusetts, focused on the development of novel therapies for mental and neurological illnesses. History Cerevel was established in October 2018. The company was formed in a collaboration between pharmaceuticals company Pfizer and private equity firm Bain Capital. In 2019, Cerevel appointed N. Anthony Coles as its chief executive officer. In 2020, Coles led Cerevel's effort to raise $445 million for brain drugs, the third largest biotech public listing at that time (after Legend Biotech and Moderna). In May 2023, Coles resigned from his position as CEO, yet retained his role as board chairman of Cerevel. In December 2023, American pharmaceutical company AbbVie announced its intention to acquire Cerevel for US$8.7 billion. The acquisition was completed in August 2024 with Cerevel becoming a subsidiary of Abbvie. Pipeline Cerevel uses novel approaches and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay, together with mood stabilizers, in the treatment of bipolar disorder. Moreover, they are also used as adjuncts in the treatment of treatment-resistant major depressive disorder. The use of antipsychotics may result in many unwanted side effects such as involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. Long-term use can produce adverse effects such as tardive dyskinesia, tardive dystonia, tardive akathisia, and brain tissue volume reduction. The long term use of antipsychotics often changes the brain both structurally and chemically in a way that can be difficult or impossible to reverse. This can lead ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Karuna Therapeutics
The Bristol-Myers Squibb Company, doing business as Bristol Myers Squibb (BMS), is an American multinational pharmaceutical company. Headquartered in Princeton, New Jersey, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the ''Fortune'' 500 list of the largest U.S. corporations. For fiscal 2022, it had a total revenue of $46.2 billion. Bristol Myers Squibb manufactures prescription pharmaceuticals and biologics in several therapeutic areas, including cancer, HIV/AIDS, cardiovascular disease, diabetes, hepatitis, rheumatoid arthritis, and psychiatric disorders. BMS's primary research and development (R&D) sites are located in Lawrence, New Jersey (formerly Squibb, near Princeton), Summit, New Jersey, formerly HQ of Celgene, New Brunswick, New Jersey; Redwood City, California; and Seville in Spain, with other sites in Devens and Cambridge, Massachusetts; Braine-l'Alleud, Belgium; Tokyo, Japan; Hyderabad; Bangalore, India and Wirral, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
