paliperidone   Click here for help

GtoPdb Ligand ID: 7258

Synonyms: 9-hydroxyrisperidone | Invega® | Ro-76477 | Ro-92670
Approved drug
paliperidone is an approved drug (FDA (2006), EMA (2007))
Compound class: Synthetic organic
Comment: Paliperidone is an atypical antipsychotic. Mechanistically it is a dopamine receptor and 5-HT2A receptor antagonist.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 4
Topological polar surface area 84.39
Molecular weight 426.21
XLogP 2.96
No. Lipinski's rules broken 0
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Canonical SMILES Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2O
Isomeric SMILES Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2O
InChI InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
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Summary of Clinical Use Click here for help
Used to treat psychotic or manic symptoms of schizophrenia.
In November 2014, the US FDA granted a supplemental New Drug Application (sNDA) for paliperidone palmitate (PubChem CID 9852746) as a treatment for schizoaffective disorder as either monotherapy or adjunctive therapy. This sNDA will be scrutinised under priority review, a mechanism whereby drugs may be approved more quickly, if they are found to offer significant improvement in the treatment of serious conditions, over currently available therapies. Following publication of results from a Phase 3 clinical trial [1], the FDA formally approved the use of paliperidone palmitate (trade named Invega Trinza) as a long-acting schizophrenia medication in May 2015. Invega Trinza has a dosing interval of three months.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
The most likely molecular mechanism of action (MMOA) of this drug is via antagonism of dopamine D2 and serotonin 5-HT2A receptors. The full MMOA remains to be determined.
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