5-HT1 Antagonists Pipeline Insights 2019

  • OI-90
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  • Published date: Apr, 2019
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  • Biopharmaceuticals
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  • 0 Pages

A group of G protein-coupled receptors (GPCRs), the serotonin (5-HT) receptors, and ligand-gated ion channels (LGICs) are found scattered in the central and peripheral nervous systems. The neurotransmitter serotonin, the natural ligand, activates 5-HT receptors and mediates both excitatory and inhibitory neurotransmission that modulates for the release of several neurotransmitters as well as several hormones. 5-HT receptors affect various biological and neurological processes such as aggression, appetite, anxiety, learning, memory, cognition, mood, sleep, and thermoregulation. Hence, 5-HT receptors are the target of various pharmaceutical drugs including antidepressants, anorectics, antipsychotics, gastroprokinetic agents, antiemetics, entactogens, and antimigraine agents. Several 5-HT receptor families and subtypes have evolved.

Market Overview

5-HT1A receptor is one of the subtypes of the serotonin (5-HT) receptor that is in presynaptic and postsynaptic regions. Activation of this receptor was elaborated in the mechanism of action of drugs including anxiolytic, antipsychotic, and antidepressant drugs. WAY 100635, BMY 7378, Lecozotan, Cyanopindolol has been used as selective 5-HT1A receptor antagonists. There found a couple of drugs for 5-HT1A receptors that will hit the market (such as buspirone and vilazodone). These are not only 5-HT1A drugs but are also found to have many other effects. Clinically active anti-depressant treatments will modify the response of 5-HT1Areceptors in many brain regions. The 5-HT1A receptor antagonists currently understudies are NRX-101 by NeuroRx for treating suicidal Bipolar Depression, Latuda by Sunovion pharmaceuticals for treating Major Depressive Disorder. It has been proposed that desensitization of 5-HT1A auto receptors after chronic treatment with antidepressant drugs is a major factor in antidepressant efficacy and will cause the delay between the commencement of treatment and the development of depressive symptoms. Minerva Neurosciences have been developing MIN-117, an antidepressant drug candidate that targets 5-HT1A receptors to address unmet medical needs in patients with Major Depressive Disorder and having anxio-depressive symptoms.

The clinical pipeline of 5-HT1 antagonists is found to have less number of studies. The 5-HT1B and 5-HT1D receptors in humans are pharmacologically differentiated from using nonselective 5-HT1B/D receptor antagonists that include ketanserin, methiothepin, and ritanserin. A novel series of benzanilides have been reported recently, and GR 127935 is the first selective 5-HT 1B/D receptor antagonists, which is a representative compound of this series displaying mixed agonist-antagonist properties. The drugs included in phase III trials of drug development are Vortioxetine and Fluoxetine developing by H. Lundbeck A/S and Takeda, Morphine sulphate, Granisetron, Brexpiprazole, Aripiprazole, Haloperidol, and Olanzapine. Drugs that inhibit the re-uptake of 5-HT, like fluoxetine, have been using clinically from many years.

The precise role of these receptors remains undefined, and the lack of selective ligands has hampered progress toward this. Physiological functions of these drugs and their receptor type interactions will be the future area of research. The interest of the key pharmaceutical companies in 5-HT1 antagonists is increased by discovering the selective and potent tools, by knowing the fact of the blockade of terminal 5-HT1 receptors by selective antagonists that has been proposed as a new approach for most of the efficient fast-acting antidepressant drugs, and by acute blockade of these 5-HT autoreceptors, which will, immediately mimic their desensitization. The limitations of existing therapies including the slow onset of action and inadequate safety and tolerability, along with many typical side effects are challenging for developing new therapeutics.

Key Developments

  • In Oct 2018, Proteus Digital Health and Otsuka expanded their global collaboration agreement for the development of aripiprazole embedded with Proteus ingestible sensor for patients suffering from severe mental illness.

  • In Feb 2019, Otsuka and Lundbeck announced that Health Canada issued a notice of compliance for brexpiprazole for using as an adjunct to antidepressants for the treatment of the major depressive disorder (MDD) in adult patients.


This Pipeline research report segments the 5-HT1 Antagonists pipeline on the basis of therapies employed (monotherapy, combination therapy, and unknown), therapeutic modality (small molecules, and unknown), RoA (oral and unknown), drugs under development (discovery, pre-clinical, phase I, phase I/II, phase II, and phase III), and recruitment status (recruiting, active not recruiting, enrolling by invitation, and undisclosed).

Some of the major market players in the research and development of 5-HT1 Antagonist drugs include Wyeth, Servier, Novartis, Mitsubishi Tanabe Pharma Corporation, Novartis, GlaxoSmithKline, AstraZeneca & list continues.

Report Description: The report covers in-depth analysis on 5-HT1 Antagonists Pipeline Insights, 2019. The report assesses the 5-HT1 Antagonists pipeline by stage of development (early development, pre-clinical, clinical and in approval), by application (anxiety, depression, major depressive disorder, mental illness, and others). In addition, the report includes key insights on other development activities, including (but not limited to) – licensing (In and Out), collaborations, acquisitions, reimbursement, patent, and regulatory designations.

The report includes in-depth company profiles of key players in 5-HT1 Antagonists Pipeline. The company profile includes key information on overview, financial highlights, product portfolio, business strategies, and key recent developments.

The report highlights information on emerging companies with potentially disruptive technologies and new market entrants.


  • Provides detailed analysis of the product pipeline structure along with forecast of the various segments and sub-segments of the 5-HT1 Antagonists Pipeline.

  • Provides a comparative analysis of key marketed products and pipeline 5-HT1 Antagonists

  • Provides key information on players involved on the 5-HT1 Antagonists Pipeline

  • Provides a complete overview of market segments and the regional outlook of 5-HT1 Antagonists Pipeline

  • Provides in-depth coverage of key news related to 5-HT1 Antagonists Pipeline, including major mergers and acquisitions and product development updates such as clinical trial progression updates and regulatory updates

Our research works on a holistic 360° approach to deliver high quality, validated and reliable information in our market reports. The Market estimation and forecasting involve the following steps:

  • Data Collation (Primary & Secondary)

  • In-house Estimation (Based on proprietary databases and Models)

  • Market Triangulation

  • Forecasting

  • Market-related information is assembled from both primary and secondary sources. 

  • Primary sources involved participants from all global stakeholders such as experts from several related industries and suppliers that have been interviewed to obtain and verify critical information as well as to assess prospects of the market. The participants included are CXOs, VPs, and managers. Plus, our in-house industry experts having decades of industry experience contribute their consulting and advisory services. 

  • Secondary sources include public sources such as regulatory frameworks, government IT spending, government demographic indicators, industry association statistics, and company publications annual reports press releases along with paid sources such as Factiva, OneSource, Bloomberg among others. 

  • Top-down and bottom-up approaches: The overall market size was used in the top-down approach to estimate the sizes of other individual submarkets (mentioned in the market segmentation by product, type of manufacturing, and disease) through percentage splits from secondary and primary research. The bottom-up approach was also implemented (wherever applicable) for data extracted from secondary research to validate the market segment revenues obtained. 


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