Routes of
administration Oral UNII X8L60BA01I | DrugBank DB09226 | |
RP-5063, also known as RP-5000, is an investigational atypical antipsychotic which is under development by Reviva Pharmaceuticals for the treatment of schizophrenia and schizoaffective disorder. Reviva Pharmaceuticals also intends to investigate RP-5063 for the treatment of bipolar disorder, major depressive disorder, psychosis/agitation associated with Alzheimer's disease, Parkinson's disease psychosis, attention deficit hyperactivity disorder (ADD/ADHD), and autism. As of May 2015, it is in phase III clinical trials for schizophrenia.
Pharmacodynamics
RP-5063 is frequently described as a so-called "dopamine-serotonin system stabilizer" due to its unique actions on the dopamine and serotonin neurotransmitter systems compared to other antipsychotics. Specifically, it acts as a partial agonist of the D2, D3, and D4 receptors and of the 5-HT1A and 5-HT2A receptors, and as an antagonist of the 5-HT6 and 5-HT7 receptors. RP-5063 has high affinity for the D2S, D2L, D3, D4.4, 5-HT1A, 5-HT2A, 5-HT7, and I H1 receptors, and moderate affinity for the D1, D5, 5-HT3, 5-HT6 receptors, the SERT, and the α1B-adrenergic receptor. It lacks significant affinity for the 5-HT1B, 5-HT2C, α2-adrenergic, and mACh receptors, as well as for the NET and DAT.