Serotonin 1A Receptor Partial Agonist Market: Competitive Landscape, Pipeline, and Market Analysis 2024

The serotonin 1A receptor or 5-HT1A receptor is a subtype of serotonin receptors or 5-HT receptors, that binds serotonin neurotransmitter, also known as 5-HT. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and the net effect of serotonin 1A receptor partial agonists is promoting serotonergic neurotransmission, to a lesser extent compared to full agonists. The modulation of serotonin signaling in the brain is thought to contribute to mood regulation, anxiety reduction, and the treatment of depressive symptoms. The mechanism of action (MOA) of Serotonin 1A Receptor Partial Agonist is that after binding to the serotonin 1A receptor, located in the central nervous system (CNS) initiates a conformational change in the receptor structure.

One of the key effects is the inhibition of adenylate cyclase, an enzyme responsible for producing cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP). By inhibiting adenylate cyclase, serotonin 1A receptor partial agonists decrease the production of cAMP, resulting in a reduction of intracellular signaling. Serotonin 1A Receptor Partial Agonists are used to treat CNS disorders, movement disorders, schizophrenia, metabolic disorders, diabetes mellitus, acute coronary syndrome, alcoholism, and collagen diseases to name a few. Increased prevalence of neurological disorders and changing lifestyles are the key drivers for the Serotonin 1A Receptor Partial Agonist market. For instance, according to the World Health Organization 2023, an estimated 3.8% of the population experience depression, including 5% of adults (4% among men and 6% among women) and 5.7% of adults older than 60 years. approximately 280 million people in the world have depression. Depression is about 50% more common among women than among men. Worldwide, more than 10% of pregnant women and women who have just given birth experience depression. Launch of newer products by the market players could seek opportunities that influence extensive research and development in Serotonin 1A Receptor Partial Agonist. For instance, Otsuka Pharmaceuticals launched Rexulti (Brexpiprazole) to treat schizophrenia. Moreover, the development of novel molecules by market players is coming up to overcome challenges in therapy. For instance, Reviva’s Brilaroxazine (RP5063) for the treatment of schizophrenia is under the various stages of clinical studies.

Serotonin 1A Receptor Partial Agonist Market Key Market Developments:

• In December 2022, AbbVie received an FDA grant for Vraylar (Cariprazine) for its expanded indication as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults.
• In May 2023, Otsuka Pharmaceuticals received an FDA grant for Rexulti (Brexpiprazole) for its expanded indication in the treatment of agitation associated with dementia due to Alzheimer’s disease.

Approved Drug Molecules and Brand Names for Serotonin 1A Receptor Partial Agonist:

•  Rexulti (Brexpiprazole)
•  Vraylar (Cariprazine)
•  Abilify Maintena (Aripiprazole Depot Formulation)
•  Viibryd (Vilazodone)
•  Sunosi (Solriamfetol)

Drugs under the Pipeline for Serotonin 1A Receptor Partial Agonist:

• Brexpiprazole QW (OPC-34712 Once Weekly)
• Eltoprazine (DU 28853)
• Hypidone Hydrochloride (HHT101)
• Abilify Asimtufii (Aripiprazole Two-Month)
• Brilaroxazine (RP5063)
• ACH-000029
• DSP-1053
• JX11502MA

Clinical Activity and Developments of Serotonin 1A Receptor Partial Agonist:

Till July 2023, more than 20 companies have approximately 17 molecules targeting the many CNS disorders. For these molecules, more than 120 clinical trials are being conducted; most are in phase-2 and phase-3 clinical trials by players across the globe. For instance,

• In March 2019, Sumitomo Pharma received FDA approval for its Sunosi (Solriamfetol) based on the 12-week, multi-center, randomized, double-blind, placebo-controlled, parallel-group study in adult patients with a diagnosis of narcolepsy according to the ICSD-3 or DSM-5 criteria.
• In March 2023, Otsuka Pharmaceutical completed phase 1b, an open-label, multiple-dose, randomized, parallel-arm, safety, tolerability, and pharmacokinetic trial of Aripiprazole intramuscular depot administered in the gluteal muscle in adult subjects with schizophrenia or bipolar I disorder.