Phase II trial evaluating the safety and efficacy of a 5-day administration of ME2136 combined with standard antiemetic therapy for the prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenic chemotherapy

Start Date16 Jul 2024

Sponsor / Collaborator-

CTR20240253

/ Active, not recruitingNot Applicable

一项评价阿塞那平透皮贴剂在健康成年人中药代动力学特征及安全性的临床研究

[Translation] A clinical study to evaluate the pharmacokinetic characteristics and safety of asenapine transdermal patch in healthy adults

主要研究目的:评价阿塞那平透皮贴剂 (ASE TTS) 单次给药与阿塞那平透皮贴剂(Secuado®)多次给药的药代动力学特征; 次要研究目的:评价使用阿塞那平透皮贴剂后受试者的安全性；评估阿塞那平透皮贴剂 (ASE TTS) 的黏附性；评估阿塞那平透皮贴剂 (ASE TTS) 的药物残留量。

[Translation]

Primary study objectives: To evaluate the pharmacokinetic characteristics of single-dose and multiple-dose asenapine transdermal patches (ASE TTS); Secondary study objectives: To evaluate the safety of subjects after using asenapine transdermal patches; To evaluate the adhesion of asenapine transdermal patches (ASE TTS); To evaluate the drug residue in asenapine transdermal patches (ASE TTS).

Start Date28 Feb 2024

Sponsor / Collaborator

LTS LOHMANN Therapie-Systeme AG

[+2]

CTR20222759

/ CompletedPhase 3

评价马来酸阿塞那平舌下片治疗急性期精神分裂症的有效性和安全性的随机、双盲、阳性对照、多中心临床试验

[Translation] A randomized, double-blind, positive-controlled, multicenter clinical trial to evaluate the efficacy and safety of asenapine maleate sublingual tablets in the treatment of acute schizophrenia

评价马来酸阿塞那平舌下片治疗急性期精神分裂症的有效性和安全性

[Translation]

To evaluate the efficacy and safety of asenapine maleate sublingual tablets in the treatment of acute schizophrenia

Start Date11 Jan 2023

Sponsor / Collaborator

Harbin Medisan Pharmaceutical Co., Ltd.

100 Clinical Results associated with Asenapine Maleate

100 Translational Medicine associated with Asenapine Maleate

100 Patents (Medical) associated with Asenapine Maleate

736

Literatures (Medical) associated with Asenapine Maleate

01 Jun 2025·PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Unraveling the Molecular Architecture of Mosquito D1‐Like Dopamine Receptors: Insights Into Ligand Binding and Structural Dynamics for Insecticide Development

Article

Author: Bhaumik, Prasenjit ; Dasgupta, Subrata

ABSTRACT:

Vector‐borne diseases pose a severe threat to human life, contributing significantly to global mortality. Understanding the structure–function relationship of the vector proteins is pivotal for effective insecticide development due to their involvement in drug resistance and disease transmission. This study reports the structural and dynamic features of D1‐like dopamine receptors (DARs) in disease‐causing mosquito species, such as Aedes aegypti, Culex quinquefasciatus, Anopheles gambiae, and Anopheles stephensi. Through molecular modeling and simulations, we describe the common structural fold of mosquito DARs within the G‐protein–coupled receptor family, highlighting the importance of an orthosteric and enlarged binding pocket. The orthosteric binding pocket, resembling a cage‐like structure, is situated ~15 Å deep within the protein, with two serine residues forming the roof and an aspartate residue, along with two conserved water molecules (W1 and W2), forming the floor. The side walls are composed of two phenylalanine residues on one side and a valine residue on the other. The antagonist binding site, an enlarged binding pocket (EBP) near the entrance cavity, can accommodate ligands of varying sizes. The binding energy of dopamine is observed to be ~2–3 kcal/mol higher than that of the antagonist molecules amitriptyline, asenapine, and flupenthixol in mosquito DARs. These antagonist molecules bind to EBP, which obstructs dopamine movement toward the active site, thereby inhibiting signal transduction. Our findings elucidate the molecular architecture of the binding pockets and the versatility of DARs in accommodating diverse ligands, providing a foundational framework for future drug and insecticide development.

01 May 2025·EUROPEAN NEUROPSYCHOPHARMACOLOGY

Antipsychotic drug dosing and study discontinuation in schizophrenia: A systematic review and dose-response meta-analysis

Review

Author: Wu, Hui ; Leucht, Stefan ; Lin, Xiao ; Tian, Jing ; Siafis, Spyridon ; Schneider-Thoma, Johannes

BACKGROUND:

High discontinuation rates compromise the effectiveness of treatment regimens for schizophrenia, because consistent medication adherence is essential for the efficacy of antipsychotics. Understanding the relationship between antipsychotic doses and discontinuation rates is important. This study explores this relationship to identify doses that maximize treatment adherence and minimize discontinuation.

METHODS:

We systematically searched multiple electronic databases for fixed-dose RCTs assessing 20 antipsychotics in patients with acute exacerbation of schizophrenia and related disorders. We analyzed dose-response relationships using a one-stage dose-response meta-analysis within a frequentist framework, employing restricted cubic splines to model the relationships. The primary outcome was discontinuation for any reason, and secondary outcomes were discontinuation due to inefficacy and side effects.

RESULTS:

Analysis of 136 trials involving 44,126 participants revealed various dose-response relationships for antipsychotics. For the primary outcome, all-cause discontinuation, amisulpride, cariprazine, olanzapine (Zyprexa), and quetiapine demonstrated U-shaped curves, indicating optimal dosing thresholds where further increases in dosage led to heightened discontinuation rates, possibly due to side effects. Aripiprazole, asenapine, brexpiprazole, clozapine, paliperidone, and risperidone (Risperdal) had plateaus, suggesting no additional benefit from increasing doses beyond specific points. For haloperidol, iloperidone, lumateperone, lurasidone, sertindole, and ziprasidone, the dose-response curves did not reach a plateau within the examined doses. Inefficacy discontinuation curves were similar to total discontinuation. Most discontinuation for side-effects curves showed sharp increases in side-effects associated with higher doses.

CONCLUSION:

Dose discontinuation curves varied between the antipsychotics and included U-shaped, monotonic, and hyperbolic patterns. Future studies should consistently present disease-related and side-effect-related dropouts due to adverse events separately.

01 May 2025·INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY

Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis

Article

Author: Zeng, Xinnian ; Lin, Tao ; Liu, Shiyan ; Xiang, Qian ; Gong, Xin ; Liu, Jiali ; Yu, Jinxin ; Zhang, Xuefeng

Dopamine (DA) is a critical molecule within the insect nervous system, known to regulate a myriad of physiological functions and instigate behavioral shifts in insects. It exerts its effects by interacting with specific dopamine receptors (DARs). In this study, three DARs cDNAs from Bactrocera dorsalis (Hendel) (Diptera: Tephritidae) (BdDOP1, BdDOP2 and BdDOP3) were cloned using molecular biology techniques. These receptors exhibited high sequence identity with their orthologous DARs, and phylogenetic analyses also clustered these receptors within their respective receptor subtype. Additionally, the high expression levels of these DARs in the head suggest their prominent role in the central nervous system of B. dorsalis. To investigate the pharmacological properties of these receptors, expression vectors for BdDOP1, BdDOP2 and BdDOP3 were constructed and expressed in HEK-293T cells. Our results demonstrated that DA and synthetic agonists activated these receptors in a dose-dependent manner, and DA activation can be competitively inhibited by various antagonists, exhibiting distinct potencies for each dopamine receptor type. Among the tested antagonists, SCH-23390, methiothepin, and metoclopramide were identified as the most potent inhibitors of BdDOP1, BdDOP2 and BdDOP3, respectively. This study provides valuable insights into the molecular and pharmacological characteristics of DARs in B. dorsalis, offering a theoretical foundation for the development of novel behavioral modulators targeting these receptors. The findings also serve as a reference for the functional analyses of DARs in other insect species.

News (Medical) associated with Asenapine Maleate

26 Aug 2024

·www.prnewswire.com

Schizophrenia Market: RISVAN's Approval Has Sparked a Competitive Race Among Pharmaceutical Companies | DelveInsight

The recent approval of Rovi Pharmaceuticals Laboratories' OKEDI/RISVAN (risperidone ISM) has spiked the competition among the other pharmaceutical companies that are developing novel therapies to improve the treatment landscape. RISVAN has the potential to become a blockbuster drug. LAS VEGAS, Aug. 26, 2024 /PRNewswire/ -- Schizophrenia is a severe mental illness affecting about 1% of Americans, cognitive functions, emotional responses, decision-making, and social interaction. Onset typically occurs in late teens to early 20s for men and late 20s to early 30s for women. Currently, as per the WHO, the vast majority of schizophrenia patients around the world are not receiving mental health care. Approximately 50% of people in mental hospitals have a schizophrenia diagnosis, and only 31.3% of people with psychosis receive specialist mental health care. As per DelveInsight analysis, in 2023 the total diagnosed prevalent cases of schizophrenia in the 7MM were found to be approximately 4 million cases out of which the US accounted for nearly 1.5 million cases. It is anticipated that these numbers will rise by 2034 due to several factors, including population growth, improved diagnostic techniques, increased awareness, and reduced stigma around mental health issues prompting more individuals to seek diagnosis, and potentially, environmental stressors contributing to a higher occurrence of the disorder. Schizophrenia treatment involves a blend of medication, psychological counseling, and social support. However, nearly one-third of patients do not respond sufficiently to standard treatments. Relapses, characterized by psychotic symptoms and functional impairments, are significant. Schizophrenia treatment mainly consists of antipsychotic medications that target dopamine neurotransmitters. Second-generation medications are favored because they lower the risk of severe side effects. Long-acting injectable antipsychotics can enhance adherence and improve treatment outcomes. High-dose regimens of specific medications may be advantageous for patients with severe, treatment-resistant schizophrenia. Additionally, hospitalization and electroconvulsive therapy might be necessary for patients who do not respond to medication therapy or during severe episodes. First-generation antipsychotics like chlorpromazine, fluphenazine, haloperidol, and perphenazine are effective in treating positive symptoms such as hallucinations and delusions but do not alleviate negative symptoms or cognitive impairments. Second-generation antipsychotics, including REXULTI/RXULTI (brexpiprazole), CAPLYTA (lumateperone), LATUDA (lurasidone hydrochloride), SAPHRIS (asenapine), ABILIFY MYCITE (aripiprazole tablets with sensor), VRAYLAR/REAGILA (cariprazine), SECUADO (asenapine), INVEGA SUSTENNA/TRINZA/HAYFERA (paliperidone palmitate), ARISTADA/ARISTADA INITIO (aripiprazole lauroxil), PERSERIS (risperidone), FANAPT (iloperidone), and LYBALVI (olanzapine and samidorphan), were developed to address both positive and negative symptoms, as well as cognitive symptoms. Although these medications typically have fewer extrapyramidal side effects, they can cause weight gain, sexual dysfunction, and other metabolic disorders. Additionally, elderly patients using FGAs and SGAs are at an increased risk of developing pneumonia. Learn more about the FDA-approved schizophrenia drugs @ Drugs for Schizophrenia Treatment REXULTI (brexpiprazole) is an oral tablet available in strengths from 0.25 mg to 4 mg, containing various inactive ingredients. While its exact mechanism of action is not fully understood, it work as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors and as an antagonist at serotonin 5-HT2A receptors. REXULTI was first approved in the US in July 2015 for use in adults with MDD and schizophrenia. In January 2022, it received FDA approval for pediatric patients aged 13–17. The EMA approved it in July 2018, and Japan approved it in tablet form in January 2018 and as an oral-disintegrating dose in August 2021. Generic versions of REXULTI have now been approved, which may affect its market presence. Janssen Pharmaceutical's INVEGA SUSTENNA/INVEGA TRINZA/INVEGA HAFYERA (paliperidone palmitate) is an SGA agent that seems to act as a D2 partial agonist and a 5-HT-2A receptor antagonist. INVEGA SUSTENNA is administered monthly, INVEGA TRINZA every three months, and INVEGA HAFYERA twice yearly. Paliperidone is a benzisoxazole derivative. In the EU and Japan, INVEGA SUSTENNA is marketed as XEPLION. In the EU, INVEGA TRINZA is sold as TREVICTA, and in Japan as XEPLION TRI. INVEGA HAFYERA is a long-acting injectable treatment administered in the upper buttocks every six months, providing continuous treatment and symptom control over this period. Additionally, the recent approval of RISVAN (Risperidone ISM) has intensified the competition in the schizophrenia treatment space. Risperidone ISM is a long-acting injectable antipsychotic created and patented by ROVI for treating schizophrenia in adults. From the first injection, it delivers immediate and sustained plasma drug levels without the need for loading doses or additional oral risperidone. This approval is based on the positive outcomes of the pivotal PRISMA-3 study, which assessed the efficacy and safety of Risperidone ISM in patients with schizophrenia. The study's findings demonstrate that the two doses tested (75 mg and 100 mg administered once monthly) successfully met the predetermined primary and secondary efficacy endpoints for treating patients with moderate to severe schizophrenia symptoms. Furthermore, OKEDI (risperidone ISM) was launched in Germany, the UK, and Spain in 2022. The approval was based on the positive results of the pivotal PRISMA-3 study on the efficacy and safety of risperidone ISM in schizophrenia patients. As per the estimates by Delveinsight analysts, this drug has blockbuster potential in the schizophrenia market with medium-fast uptake. To know more about schizophrenia treatment options, visit @ New Treatment for Schizophrenia The schizophrenia market is crowded with so many companies working in the domain. Various potential therapies that are projected to enter during the forecast period include Boehringer Ingelheim's Iclepertin (BI-425809), Sumitomo Pharma/Otsuka's Ulotaront (SEP-363856), Reviva Pharmaceuticals' Brilaroxazine (RP5063), Minerva Neurosciences/Mitsubishi Tanabe Pharma's Roluperidone (MIN-101/MT-210), Karuna Therapeutics (Bristol Myers Squibb)/Royalty Pharma's KarXT (xanomeline-trospium), ACADIA Pharmaceuticals' NUPLAZID (pimavanserin), Teva Pharmaceutical/MedinCell/Royalty Pharma's Olanzapine LAI (mdc-TJK/TV-44749), Neurocrine Biosciences/Mitsubishi Tanabe Pharma's Valbenazine (NBI-98854), Lyndra Therapeutics' LYN-005 (long-acting oral risperidone), Newron Pharmaceuticals' Evenamide (NW-3509), Luye Pharma's LY03010 (ER paliperidone palmitate), and others. Discover which therapies are expected to grab major schizophrenia market share @ Schizophrenia Market Report Iclepertin (BI 425809) is an investigational drug and a glycine transporter 1 (GlyT1) inhibitor aimed at addressing the brain biology related to cognitive symptoms in schizophrenia (CIAS). Abnormalities in glutamatergic signaling downstream of neuronal NMDA receptors contribute to cognitive impairment in this condition. Enhancing NMDA receptor function could potentially improve synaptic plasticity and cognition. Glycine, an essential NMDA receptor co-agonist, is modulated by glycine transporters GlyT-1 and GlyT-2, which are located in presynaptic and astrocyte membranes. These transporters regulate glycine levels by taking it up into nerve terminals and adjacent glial cells, affecting synaptic cleft glycine concentration. By inhibiting these transporters, BI 425809 aims to increase glycine levels, thereby modulating NMDA receptor function. Administered orally, this potent and selective GlyT1 inhibitor is also under investigation for Alzheimer's disease. However, early 2020 Phase II trial results did not support its continued development for this indication, and the focus has now shifted to schizophrenia, with multiple Phase III trials currently underway. Since schizophrenia, patients frequently ignore certain symptoms, such as cognitive impairment. Therefore, if approved, BI-425809 will be the first approved pharmacotherapy for the treatment of CIAS. Ulotaront (SEP-363856), developed by Sumitomo Pharma and Otsuka Pharmaceuticals, is a trace amine-associated receptor 1 (TAAR1) agonist with serotonin 5-HT1A agonist activity. It is a small-molecule oral agent that does not bind to dopamine D2 or serotonin 5-HT2A receptors. Sunovion discovered Ulotaront in collaboration with PsychoGenics using the in vivo phenotypic SmartCube platform and associated artificial intelligence algorithms. Ulotaront is currently in late-stage development for schizophrenia and generalized anxiety disorder (GAD) in Japan and as an adjunctive treatment for major depressive disorder, schizophrenia, and GAD in the US. Top-line results from Phase III DIAMOND 1 and DIAMOND 2 trials in schizophrenia have been released, but the Phase III DIAMOND 3 trial in the US has been halted. Sumitomo Pharma has also stopped a Phase III trial for schizophrenia in Japan and another Phase II/III trial in China, Japan, Taiwan, and the Philippines, citing business strategy reasons. Despite this, two Phase III trials are still ongoing. Recently, Otsuka and Sumitomo revised their licensing agreement, excluding SEP-4199 and SEP-378614. Under this revision, Otsuka gained exclusive rights from SMPA to develop, manufacture, and commercialize ulotaront worldwide. If Otsuka successfully develops and commercializes ulotaront, they will pay up to 30 million USD (approximately 4.5 billion yen) in milestones, along with royalties based on sales, without any upfront payment. Starting January 2024, Otsuka will cover the full cost of studies conducted by both Sumitomo Pharma Group and Otsuka, except for certain studies. KarXT (xanomeline–trospium) is an oral modulator targeting muscarinic receptors found in both the central nervous system (CNS) and various peripheral tissues. This proprietary product combines xanomeline, a novel muscarinic agonist, with trospium, an approved muscarinic antagonist, to preferentially stimulate muscarinic receptors in the CNS. As a dual M1/M4 muscarinic acetylcholine receptor agonist, KarXT aims to improve the positive, negative, and cognitive symptoms of schizophrenia. The US FDA has accepted Karuna Therapeutics' NDA for KarXT for adult schizophrenia treatment, with a PDUFA date of September 26, 2024. Additionally, KarXT is undergoing multiple Phase III trials as an adjunctive treatment with standard-of-care agents for schizophrenia and is being evaluated for psychosis treatment in Alzheimer's disease patients. Following Bristol Myers Squibb's acquisition of Karuna Therapeutics, Karuna is now a wholly-owned subsidiary of BMS. At the Annual Congress of the Schizophrenia International Research Society (SIRS) in April 2024 in Italy, BMS presented promising results from the latest interim analysis of the Phase III EMERGENT-4 open-label extension trial, showing KarXT's efficacy in reducing symptoms in adults with schizophrenia. BMS plans to continue discussions with the US FDA and will release more data from the EMERGENT program later this year. Discover more about drugs for schizophrenia in development @ Schizophrenia Clinical Trials The anticipated launch of these emerging therapies for schizophrenia are poised to transform the market landscape in the coming years. As these cutting-edge therapies continue to mature and gain regulatory approval, they are expected to reshape the schizophrenia market landscape, offering new standards of care and unlocking opportunities for medical innovation and economic growth. DelveInsight estimates that the market size for schizophrenia is expected to grow from USD 2.6 billion in 2023 with a significant CAGR by 2034. This growth can be attributed to the introduction of upcoming therapies and the rising prevalence of the disease. The anticipated launch of these therapies is also expected to attract new entrants to the Schizophrenia market, resulting in increased competition and innovation. DelveInsight's latest published market report titled as Schizophrenia Market Insight, Epidemiology, and Market Forecast – 2034 will help you to discover which market leader is going to capture the largest market share. The report provides comprehensive insights into the schizophrenia country-specific treatment guidelines, patient pool analysis, and epidemiology forecast to help understand the key opportunities and assess the market's underlying potential. The schizophrenia market report proffers epidemiological analysis for the study period 2020–2034 in the 7MM segmented into: Total Prevalent Cases of Schizophrenia Total Diagnosed Prevalent Cases of Schizophrenia Gender-specific Diagnosed Prevalent Cases of Schizophrenia Severity-specific Diagnosed Prevalent Cases of Schizophrenia The report provides an edge while developing business strategies by understanding trends shaping and driving the 7MM schizophrenia market. Highlights include: 11-year Forecast 7MM Analysis Epidemiology-based Market Forecasting Historical and Forecasted Market Analysis upto 2034 Emerging Drug Market Uptake Peak Sales Analysis Key Cross Competition Analysis Industry Expert's Opinion Access and Reimbursement Download this schizophrenia market report to assess the epidemiology forecasts, understand the patient journeys, know KOLs' opinions about the upcoming treatment paradigms, and determine the factors contributing to the shift in the schizophrenia market. Also, stay abreast of the mitigating factors to improve your market position in the schizophrenia therapeutic space. Related Reports Schizophrenia Pipeline Schizophrenia Pipeline Insight – 2024 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key schizophrenia companies, including Otsuka Pharmaceutical Development & Commercialization, Inc., Gedeon Richter Ltd., Lyndra Therapeutics, Neurocrine Bioscience, Takeda Pharmaceutical Company, Memory Pharmaceuticals, Hoffmann-La Roche, Neurocrine Biosciences, Boehringer Ingelheim, Meiji Seika Pharma Co., Ltd., SK Life Science, Inc., Alkermes, Inc. , Solvay Pharmaceuticals, Mitsubishi Tanabe Pharma Corporation, SyneuRx International (Taiwan) Corp, BioXcel Therapeutics Inc, Cognitive Research Corporation, Amarex Clinical Research, Forum Pharmaceuticals Inc, Amneal Pharmaceuticals, LLC, Recognify Life Sciences, Accutest Research Laboratories (I) Pvt. Ltd., Eli Lilly and Company, Johnson & Johnson Pharmaceutical Research & Development, L.L.C, Janssen, LP, Delpor, Inc., Jiangsu Hansoh Pharmaceutical, Cerevel Therapeutics, LLC, Zogenix, Inc., Luye Pharma, Reviva Pharmaceuticals, Alkermes, Inc., Karuna Therapeutics, Autifony Therapeutics, Neumora Therapeutics, Adex Therapeutics, among others. Schizophrenia Epidemiology Forecast Schizophrenia Epidemiology Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, and schizophrenia epidemiology trends. Dementia Market Dementia Market Insights, Epidemiology, and Market Forecast – 2032 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key dementia companies, including Hoffmann-La Roche, Forest Laboratories, Inc., Janssen Pharmaceuticals, Inc., Merck and Co., Inc., Novartis, among others. Bipolar Depression Market Bipolar Depression Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key bipolar depression companies, including Intra-Cellular Therapies, Sunovion Pharmaceuticals, COMPASS Pathways, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP

Phase 3Phase 2Clinical ResultDrug ApprovalLicense out/in

09 Jan 2024

·synapse.patsnap.com

D2 receptor antagonists: What They Are and How to Keep Up with the Latest Advances

The D2 receptor is a type of dopamine receptor found in the human body. It plays a crucial role in various physiological and neurological processes. As a G-protein coupled receptor, the D2 receptor is involved in the regulation of dopamine neurotransmission, which affects mood, motivation, and reward. Dysfunction of the D2 receptor has been implicated in several psychiatric disorders, including schizophrenia and addiction. Additionally, the D2 receptor is a target for antipsychotic medications, which work by blocking its activity to alleviate symptoms associated with psychosis. Understanding the role of the D2 receptor is essential for developing therapeutic interventions for psychiatric and neurological conditions. The analysis of the target D2 receptor reveals a competitive landscape with multiple companies making progress in the development of drugs. Johnson & Johnson, Mitsubishi Chemical Group Corp., Novartis AG, Sanofi, and Viatris Inc. have shown significant growth and have drugs approved for the target. Schizophrenia, bipolar disorder, and bipolar I disorder are the most common indications for approved drugs. Small molecule drugs are progressing rapidly, with intense competition from biosimilars. The United States, Japan, and China are the leading countries in the development of drugs targeting the D2 receptor, with China showing notable progress. Overall, the target D2 receptor presents opportunities for further research and development in the pharmaceutical industry. How do they work?D2 receptor antagonists are a type of medication that block or inhibit the activity of the D2 receptors in the brain. D2 receptors are a subtype of dopamine receptors, which are involved in various neurological processes. By antagonizing or blocking the D2 receptors, these medications can modulate the effects of dopamine in the brain. From a biomedical perspective, D2 receptor antagonists are commonly used in the treatment of psychiatric conditions such as schizophrenia and bipolar disorder. In these disorders, there is an imbalance of dopamine activity in the brain, and D2 receptor antagonists help to reduce the excessive dopamine signaling. By blocking the D2 receptors, these medications can help alleviate symptoms such as hallucinations, delusions, and mood disturbances. It is important to note that D2 receptor antagonists may also have side effects due to their broader effects on dopamine signaling. These can include movement disorders, such as parkinsonism, as well as metabolic changes and hormonal imbalances. Therefore, the use of D2 receptor antagonists requires careful monitoring and consideration of the potential risks and benefits for each individual patient. List of D2 receptor AntagonistsThe currently marketed D2 receptor antagonists include: Samidorphan/olanzapineLumateperone TosylateAripiprazole LauroxilCariprazine hydrochlorideBrexpiprazoleLoxapineDA-9701Lurasidone HydrochlorideAsenapine MaleatePaliperidone PalmitateFor more information, please click on the image below. What are D2 receptor antagonists used for?D2 receptor antagonists are commonly used in the treatment of psychiatric conditions such as schizophrenia and bipolar disorder. For more information, please click on the image below to log in and search. How to obtain the latest development progress of D2 receptor antagonists?In the Synapse database, you can keep abreast of the latest research and development advances of D2 receptor antagonists anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

13 Jun 2022

·www.biospace.com

Cortexyme Appoints June Bray to its Board of Directors

June 13, 2022 12:00 UTC SOUTH SAN FRANCISCO, Calif.--(BUSINESS WIRE)-- Cortexyme, Inc. (Nasdaq: CRTX), a clinical-stage biopharmaceutical company focused on rare and degenerative diseases, today announced the appointment of June Bray, a pharmaceutical industry veteran and global drug development and regulatory process expert, to the company’s Board of Directors. “We are very pleased to welcome a seasoned pharmaceutical and global regulatory expert of June Bray’s caliber to our Board of Directors,” said David Lamond, chairperson of Cortexyme’s Board of Directors. “With more than four decades of pharmaceutical industry experience, we look forward to her valuable contribution and perspective across multiple therapeutic areas.” “I am excited to join Cortexyme’s Board of Directors as the company works to efficiently and effectively advance its current clinical stage therapeutics, in addition to expanding its development pipeline in strategic ways,” said June Bray. “I look forward to supporting the new leadership team as they work to establish a clear roadmap for driving the company’s clinical stage and discovery pipeline, and in the evaluation of new business development opportunities.” To the Cortexyme Board of Directors, Ms. Bray brings more than forty years of extensive U.S. and global regulatory experience in the healthcare industry and a proven track record of successful regulatory interactions with health authorities which have led to the approval of 32 NDAs in the U.S. and multiple international approvals. She most recently served as Senior Vice President, Global Regulatory Affairs and Medical Writing at Allergan, where she was responsible for regulatory strategies on development projects and lifecycle management in all therapeutic areas, including psychiatry and neurology. During her tenure, she led numerous NDA approvals, including Namenda XR®, Namzaric®, Vraylar®, and Ubrelvy®. Previously, Ms. Bray served as Vice President, Regulatory Affairs at Organon (now Merck), where she led regulatory activities for development and marketed products, including the NDA for Saprhis® (asenapine) for the treatment of schizophrenia and bipolar disorder. Earlier in her career, Ms. Bray held numerous roles of increasing responsibility over a 25-year period at Berlex Laboratories, Inc. (now Bayer HealthCare Pharmaceuticals). She began her pharmaceutical career in sterile manufacturing at Hoechst-Roussel Pharmaceuticals (now Sanofi-Aventis). Ms. Bray holds a B.S. in Pharmacy from the University of Rhode Island and an M.B.A in Pharmaceutical Marketing from Fairleigh Dickinson University. About Cortexyme Cortexyme, Inc. (Nasdaq: CRTX) is a clinical stage biopharmaceutical company focused on rare and degenerative diseases. The company’s innovative pipeline includes a precision bone growth molecule and drug-targeting platform to treat rare skeletal diseases, bone cancer and injury, in addition to small molecule therapeutics targeting the infectious pathogen P. gingivalis’ role in degenerative disease progression, including for indications such as periodontal disease, oral potentially malignant disorders, and Alzheimer’s disease, among others. To learn more about Cortexyme, visit or follow @Cortexyme on Twitter.

Small molecular drug

100 Deals associated with Asenapine Maleate

External Link

KEGG	Wiki	ATC	Drug Bank
D02995	Asenapine Maleate	N05AH05	DB06216

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Bipolar I disorder	European Union	Organon NV	01 Sep 2010
Bipolar I disorder	Iceland	Organon NV	01 Sep 2010
Bipolar I disorder	Liechtenstein	Organon NV	01 Sep 2010
Bipolar I disorder	Norway	Organon NV	01 Sep 2010
Mania	European Union	Organon NV	01 Sep 2010
Mania	Iceland	Organon NV	01 Sep 2010
Mania	Liechtenstein	Organon NV	01 Sep 2010
Mania	Norway	Organon NV	01 Sep 2010
Bipolar Disorder	United States	Allergan Sales LLC	13 Aug 2009
Schizophrenia	United States	Allergan Sales LLC	13 Aug 2009

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Stuttering	Phase 3	United States	Merck Sharp & Dohme Corp.	01 Sep 2012
Schizophrenia, Treatment-Resistant	Phase 3	-	Organon & Co.	05 Apr 2011
Schizophrenia, Disorganized	Phase 3	-	Organon & Co.	28 Sep 2010
Psychotic Disorders	Phase 3	-	Organon & Co.	01 Feb 2006
Acute schizophrenia	Phase 3	-	Organon & Co.	01 Apr 2005
Paranoid Schizophrenia	Phase 3	-	Organon & Co.	01 Dec 2004
Schizoaffective disorder	Phase 3	-	Organon & Co.	04 Sep 2003
Depressive Disorder, Major	Phase 2	-	Organon & Co.	29 Jun 2005

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02876900 (HP-3070, CTgov)	Phase 3	Schizophrenia	617	Placebo+Low Dose Asenapine maleate transdermal patch (Low Dose Asenapine Maleate Patch)	lqlsmonqnc(afqzszzpwj) = xsgfivkfmh zbptfxbkhq (zmdkylieoh, 1.158) View more	-	27 Mar 2020
				Placebo+High Dose Asenapine maleate transdermal patch (High Dose Asenapine Maleate Patch)	lqlsmonqnc(afqzszzpwj) = qjzbwyvsex zbptfxbkhq (zmdkylieoh, 1.162) View more
NCT00145470 (P05844 \| A7501008, CTgov)	Phase 3	Bipolar Disorder \| Bipolar I disorder	326	Placebo (Placebo)	xrpfpbrdfm(rtceizogsb) = uqppqgvebc eryqdvmcpu (xwelfarncv, 0.45) View more	-	16 Sep 2019
				Asenapine (Asenapine)	xrpfpbrdfm(rtceizogsb) = lpukqbvrvm eryqdvmcpu (xwelfarncv, 0.46) View more
NCT01396291 (P06384, Pubmed \| Am J Psychiatry) Manual	Phase 3	Bipolar I disorder Maintenance	253	Asenapine	lidaxtssxo(cfigxvkdbr) = statistically significantly longer for asenapine- than placebo-treated subjects. nkvejtezns (qqxuasdgfp ) View more	Positive	01 Jan 2018
				Placebo
NCT01617187 (Pubmed \| CNS Spectr)	Phase 3	Acute schizophrenia	360	Asenapine 5 mg bid	enouhzczjn(eadgwhxljn): points = -5.5 (95% CI, -10.1 to -1.0), P-Value = 0.0356	Positive	01 Aug 2017
				Placebo
NCT01349907 (P05898, Pubmed \| Paediatr Drugs)	Phase 3	Bipolar I disorder	321	Asenapine	yeyrxlayfj(tbsrzofjub) = 34.8 % of patients experienced clinically significant weight gain (≥7 % increase) hmujsfibkr (frhcvfithh ) View more	-	01 Oct 2016
NCT01098110 (Pubmed \| Psychopharmacology (Berl))	Phase 3	Acute schizophrenia	532	Asenapine 5 mg bid	mscqqvilbg(efwlbzadvr) = uvcffmlqhr eofaknbrlg (ddxyefalog, ±2.65)	Positive	01 Jul 2016
				Asenapine 10 mg bid	mscqqvilbg(efwlbzadvr) = jguelatwye eofaknbrlg (ddxyefalog, ±2.89)
NCT01400113 (CTgov)	Phase 4	Agitation	120	Asenapine (Asenapine)	qjcidlejqo(pitsqijgtt) = vxsqtqvhhu opdoozniid (gtoekvpcem, ogaplzbrzg - jpcibdquuz) View more	-	16 May 2016
				Placebo (Placebo)	qjcidlejqo(pitsqijgtt) = jwaknbebbc opdoozniid (gtoekvpcem, mpixhfzzdq - mmjwshgxve) View more
NCT01244815 \| NCT01349907 (Efficacy and Safety of Asenapine Treatment for Pediatric Bipolar Disorder, Pubmed \| J Am Acad Child Adolesc Psychiatry)	Phase 3	Bipolar I disorder	403	Placebo	gdvfnyucsz(tiszkogrwn) = iiljwhxqlr nfapacmvtp (vdzgeocwjj ) View more	Positive	01 Dec 2015
				Asenapine 2.5 mg b.i.d.	iujucrouhx(lqclijevdm) = zfxpxglyyu vktsobhqyr (alecdidsac ) View more
NCT01670019 (CTgov)	Phase 4	Depressive Disorder, Major	46	Asenapine (Asenapine 5-20 mg Daily)	xvvnzxjkem(aiefpwykra) = judvknnfvg djsmekawom (jwixoxtgfl, 9.73) View more	-	01 Oct 2015
				Placebo 1-4 tablets daily (Placebo 1-4 Tablets Daily)	xvvnzxjkem(aiefpwykra) = xtilkfqxyc djsmekawom (jwixoxtgfl, 11.82) View more
NCT01190267 (P05897, Pubmed \| J Child Adolesc Psychopharmacol) Manual	Phase 3	Schizophrenia	193	Asenapine	rajmmrulkb(hfnduuphdf) = xrnrklcprt qtlsdivcnl (qyhpplqjhk )	Positive	01 Jun 2015
				Placebo	rajmmrulkb(hfnduuphdf) = yilhzsitws qtlsdivcnl (qyhpplqjhk )

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