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

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- GABA_A, GABA_B, and GABA_C. GABA_A are pentameric receptors activation of which cause anionic influx into the neuron resulting in hyperpolarization of the cell membrane.  GABA_A is widely expressed in the peripheral and the central nervous system. GABA_A 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 GABA_A 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 GABA_A 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 GABA_A 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 GABA_A 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 GABA_A 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.