5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. Serotonin 2B receptors are a subtype of serotonin (5-hydroxytryptamine or 5-HT) receptors, which are G-protein coupled receptors found in various tissues throughout the body. The 5-HT2B receptors are primarily located in the cardiovascular system, gastrointestinal tract, and central nervous system. Their activation is associated with various physiological responses, including vascular smooth muscle contraction, gut motility, and neurotransmission.
Antagonists of the serotonin 2B receptor are drugs that bind to these receptors without activating them, effectively blocking the binding of serotonin or other agonists. By doing so, they prevent the downstream signaling cascade that would occur upon receptor activation. Serotonin 2B Receptor Antagonists have been identified as an effective therapeutic strategy for CNS disorders, psychotic disorders, schizophrenia, obesity metabolic syndrome, behavioral symptoms, and depression to name a few. The increased prevalence of neurological diseases is the key driver for the Serotonin 2B Receptor Antagonists market. For instance, the World Health Organization, estimated schizophrenia affect around 20 million people globally by 2021. The launch of newer products by the market players could seek opportunities that influence extensive research and development in Serotonin 2B Receptor Antagonists. For instance, AbbVie launched Vraylar (Cariprazine) to treat bipolar disorders. Moreover, to overcome difficulties in therapy, various market players are developing innovative compounds. For instance, AnaMar’s AM 1476 for the indication of systemic scleroderma is under the various stages of clinical studies.
Serotonin 2B Receptor Antagonists Market Key Developments:
Approved Drug Molecules and Brand Names for Serotonin 2B Receptor Antagonists:
Vraylar (Cariprazine)
Drugs under the Pipeline for Serotonin 2B Receptor Antagonists:
Clinical Activity and Developments of Serotonin 2B Receptor Antagonists:
Till July 2023, more than 10 companies have approximately 10 molecules targeting several CNS diseases. For these molecules, more than 30 clinical trials are being conducted; most are in phase-2 and phase-3 clinical trials by players across the globe. For instance,
Molecule Name |
Number of Studies |
Metadoxine Extended-Release (MG01CI) |
16 |
Brilaroxazine (RP5063) |
13 |
AM 1476 |
12 |
VHX-896 |
10 |
XC101-D13H |
6 |
The molecules such as Vraylar (Cariprazine) were developed by Abbvie, for the treatment of schizophrenia, manic or mixed episodes associated with bipolar I disorder, and for depressive episodes associated with bipolar I disorder (bipolar depression) in adults, and adjunctive therapy to antidepressants for the treatment of MDD in adults. Moreover, Reviva’s Brilaroxazine (RP5063) for the indication of Schizophrenia, Idiopathic pulmonary fibrosis, and Pulmonary arterial hypertension is under clinical development.
Vraylar (Cariprazine) is the only few FDA-approved Serotonin 2B Receptor Antagonists.
Global Vraylar (Cariprazine) net revenues were USD 565 million in the fourth quarter of FY 2022.
Major market players include Mitsubishi Tanabe Recordati, Gedeon Richter, AbbVie, and Arcturus Therapeutics are a few leading market players.
Major Indications for Serotonin 2B Receptor Antagonists are used to treat CNS disorders, psychotic disorders, schizophrenia, obesity metabolic syndrome, behavioral symptoms, and depression to name a few.
There are a total of 6 molecules that are in Phase-1, Phase-2, and Phase-3 clinical development.