Dopamine receptor D2 (DRD2) is a protein-coupled by a G protein-coupled receptor. DRD2 autoreceptor activation protects dopamine neurons from cell death, and D2R mediates cognitive flexibility in humans. DRD2 partial agonists act by mediating an intermediate level of dopaminergic neuronal tone between full agonist and antagonist of the D2 receptor, and the partial agonism allows the drugs to stimulate D2 receptors under low dopamine conditions while attenuating their activation when dopamine levels are high. DRD2 Partial Agonists are indicated for DRD1 antagonists are used in the treatment of schizophrenia, management of acute manic or mixed episodes in patients with bipolar I disorder, major depression, post-traumatic stress disorder, generalized anxiety disorder, psychosis associated with Parkinson’s disease, and others. Gedeon Richter, BMS, AbbVie, Seelos Therapeutics, Otsuka Pharmaceutical, Jiangsu Kanion Pharma, and Reviva Pharmaceuticals are major players in the DRD2 partial agonists market.
Approved Drug Molecules and Brand Names for DRD2 Partial Agonists:
Drugs under the Pipeline for DRD2 Partial Agonists:
Key Market Developments:
Clinical Activity and Developments of DRD2 Partial Agonists:
Currently, there are 12 drug products in the DRD2 partial agonists, including seven approved drug products and the rest of them are in the clinical development phases.
Molecule Name |
Number of Studies |
Pardoprunox (SLV-308) |
13 |
Aplindore (SLS-006) |
4 |
TPN-672 |
2 |
Brilaroxazine (RP5063) |
2 |
JX11502MA |
1 |
DRD2 partial agonists such as Aripiprazole, Cariprazine, and Brexpiprazole are indicated in the treatment of conditions such as autistic disorder, bipolar disorders, Tourette’s syndrome, major depressive disorder, and Schizophrenia. DRD2 partial agonists are also in the clinical investigational phases for agitation, pervasive child development disorders, post-traumatic stress disorders, attention-deficit hyperactivity disorder, and others.
Aripiprazole, Rexulti (Brexpiprazole), Vraylar (Cariprazine), and Abilify Maintena (Aripiprazole depot formulation) are some of the approved DRD2 partial agonists.
Gedeon Richter, BMS, AbbVie, Seelos Therapeutics, Otsuka Pharmaceutical, Jiangsu Kanion Pharma, and Reviva Pharmaceuticals are some of the major players in the DRD2 partial agonists market.
Major indications for DRD2 partial agonists are autistic disorder, bipolar disorders, Tourette’s syndrome, major depressive disorder, and Schizophrenia.
There are a total of five molecules in the clinical development phases for DRD2 partial agonists.