GABAA Receptor Agonists Market: Competitive Landscape, Pipeline, and Market Analysis 2023

Purchase Option

$ 4400
$ 6600
$ 8900

GABA, which stands for Gamma-aminobutyric acid, is an inhibitory neurotransmitter in the human body. GABA is one of the most important neurotransmitters that regulate mood and muscle contracture. The precursor of GABA is glutamine which synthesizes GABA in the presynaptic neuron. It is mainly of 3 types- GABAA, GABAB, and GABAC. GABAA are pentameric receptors activation of which cause anionic influx into the neuron resulting in hyperpolarization of the cell membrane.  GABAA is widely expressed in the peripheral and the central nervous system. GABAA mediates anesthetic, sedative, and analgesic effects by interacting with its substrate.  These agonists are therefore used as short-acting anesthetics like propofol, analgesics, and antispasmodics like diazepam in insomnia like zolpidem and others. The development of new and novel molecules by the market players is imminent.  Extensive research is being conducted globally to discover new and novel molecules for GABAA agonists, like Zolpidem, used for insomniac patients. The development and launch of new products will thus increase the market’s revenue in the forecasted years. According to the 2023 WHO report on Epilepsy, there are about 50 million people affected with it globally. 5 million people are diagnosed with Epilepsy each year and there is an urgent need for proper treatment and help for these patients. The prevalence of the disease has been on the rise for many years, driving the market’s growth.

A number of these inhibitors are in the market, while many are in ongoing clinical trials. Many companies have various products in their pipelines, with 48 products in different stages of clinical trials. 21 products in Phase 4, 10 in Phase 3, 9 in Phase 2, and 4 in Phase 1 of the clinical trials.

Key Developments of GABAA Receptor Agonists

  • In March 2021, the EU approved Byfavo (remimazolam) for patients undergoing colonoscopy or Bronchoscopy.
  • In July 2020, FDA approved Byfavo (remimazolam) for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.
  • In January 2020, the FDA approved Valtoco (diazepam intranasal) for treating acute, intermittent, stereotypic episodes of frequent seizures in patients older than six years of age.
  • In August 2018, FDA approved Diacomit (stiripentol) indicated for the treatment of seizures associated with Dravet syndrome in patients 2 years of age and older taking clobazam. Its exclusivity will end in August 2025.
  • In September 2018, FDA approved Seizalam (midazolam intramuscular) for the treatment of patients with Status Epilepticus.

Approved molecules of GABAA Receptor Agonists

  • ByFavo (remimazolam)
  • ciprofol injectable emulsion (HSK3486)
  • Qsymia (topiramate/phentermine)
  • remimazolam tosylate (HR-7056)
  • Diacomit (stiripentol)
  • Seizalam (midazolam intramuscular)
  • Lendormin (brotizolam)
  • Valtoco (diazepam intranasal)
  • Ozalin (midazolam)
  • Epistatus (midazolam oromucosal solution)

Drugs in the Pipeline of GABAA Receptor Agonists

  • Darigabat (CVL-865)
  • Gaboxadol (OV101)
  • Adlea (Capsaicin)
  • Padsevonil (UCB0942)
  • Staccato Alprazolam (AZ-002)
  • Metyrapone/Oxazepam (EMB-001)
  • Diastat (Diazepam Rectal Gel)
  • BL-1020
  • Nayzilam (Midazolam Intranasal)
  • Libervant (Diazepam Buccal Film)
  • Diphenhydramine/Lorazepam/Zolpidem (SM-1)
  • Intermezzo (Zolpidem)
  • Acamprosate Controlled-Release (SNC-102)
  • Midazolam/Ketamine Sublingual Tablet (MELT-300)
  • Zolpidem Hemitartarate
  • EVT201
  • Vanquix (Diazepam Auto-Injector)
  • Cudafol (Captisol-Enabled Propofol)
  • Midazolam Injection
  • PF0713
  • Zaleplon GR (Zaleplon)
  • Clonazepam Intranasal (JZP-8)
  • Lorazepam Extended-Release (EDG004)
  • Staccato Zaleplon (AZ-007)

Clinical Activity and Developments of GABAA Receptor Agonists

As of July 2023, 48 companies have approximately 46 products for 301 diseases. For these diseases, 395 trials are being conducted by players globally. For instance,

  • In April 2023, Vivus LLC completed a Phase 4 clinical trial to compare the effects of VI-0521, Phentermine, and placebo on ambulatory blood pressure in overweight or obese patients.
  • Tianjin Nankai Hospital is conducting a Phase 4 clinical trial to determine the median effective dose of Remimazolam for Duodenoscopy insertion during ERCP with Alfentanil which was expected to complete by December 2021.
  • The University of Cincinnati is conducting a Phase 4 clinical trial to explore the effects on responsive neurostimulator activity after intranasal administration of a single dose of Valtoco to people with Epilepsy.

Molecule name

Number of studies

ciprofol injectable emulsion (HSK3486)


Qsymia (topiramate/phentermine)


remimazolam tosylate (HR-7056)


Diacomit (stiripentol)


ByFavo (remimazolam)


Target Indication Analysis of GABAA Receptor Agonists

Drugs like ByFavo (remimazolam) and Seizalam (midazolam intramuscular) have been approved by the FDA and other regulatory agencies for the treatment of various diseases. Byfavo acts as an agonist of GABAA in the brain and is indicated as a sedative and general anesthetic in procedures lasting 30 minutes or less. Hence, it finds use in dentistry, minor surgeries, and other surgical procedures. Seizalam has a similar mechanism of action as Byfavo and binds with the GABA receptor. It is indicated for the treatment of Status Epilepticus in adults. GABAA agonists are used in many indications such as Mood Disorders, Short-term Insomnia, Chronic Insomnia, Dyssomnias, Sleep Disorders, Anxiety, Epilepsy, etc.  

Frequently Asked Questions

ByFavo (remimazolam), ciprofol injectable emulsion (HSK3486), Qsymia (topiramate/phentermine), remimazolam tosylate (HR-7056), and Diacomit (stiripentol) are approved by various regulatory agencies.

These are used as sedatives, short-acting general anesthetics, Epilepsy, Mood Disorders, Short-term Insomnia, Chronic Insomnia, Anxiety, Epilepsy, and others.

PAION, Cosmo Pharma, Mundipharma, Pharmascience, and Eagle Pharmaceutical are some of the major market players for GABA A Receptor Agonists.

Rising incidence of diseases, improvement in technologies, development of new treatment lines in the market, and rising incidence of mental and sleep disorders are the key opportunities for GABAA Receptor Agonists in the market.

Key Features of the Reports

  • The report provides granular level information about the market size, regional market share, historic market (2019-2023), and forecast (2024-2030)
  • The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
  • The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
  • The report tracks recent innovations, key developments, and start-up details that are actively working in the market
  • The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
  • Cosmo Pharma
  • Mundipharma
  • Pharmascience
  • Eagle Pharmaceutical
  • Haisco
  • IEH Biopharma
  • Alvogen
  • Ovid Therapeutics
  • Angelini Group
  • Healx
  • Jiangsu Hengrui Pharma
  • Arcion
  • Centrexion Therapeutics
  • Biocodex
  • Meiji Seika
  • Cerevel Therapeutics
  • UCB
  • Pfizer
  • Boehringer Ingelheim
  • Embera NeuroTherapeutics
  • Bausch Health
  • BioLineRx
  • Neurelis
  • Aquestive
  • Eusol Biotech
  • Paratek
  • Primex Pharma
  • Sintetica
  • Synchroneuron
  • Melt Pharma
  • Biolab Pharma
  • Evotec
  • Zhejiang Jingxin Pharma
  • Cuda Pharma
  • Ligand Pharmaceuticals
  • Veriton Pharma
  • Rafa
  • Ensysce Biosciences
  • Indaptus Therapeutics
  • Jazz Pharmaceuticals
  • Edgemont Pharma

Adjacent Markets