Iloperidone
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| Trade names | Fanapt, Zomaril |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a609026 |
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Oral, injection |
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| Pharmacokinetic data | |
| Bioavailability | 96% (oral; Tmax = 2–4 hours) |
| Protein binding | ~97% |
| Metabolism | Hepatic (CYP2D6-mediated hydroxylation and CYP3A4-mediated O-demethylation) |
| Biological half-life | 18–33 hours |
| Excretion | urine (45.1–58.2%) and feces (19.9–22.1%) |
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| ECHA InfoCard | 100.106.441 |
| Chemical and physical data | |
| Formula | C24H27FN2O4 |
| Molar mass | 426.481g/mol |
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Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia.
It was approved by the U.S. Food and Drug Administration (FDA) for use in the United States on May 6, 2009.
Iloperidone is a monoamine directed towards acting upon and antagonizing specific neurotransmitters, particularly multiple dopamine and serotonin receptor subtypes. It is considered an ‘atypical’ antipsychotic because it displays serotonin receptor antagonism, similar to other atypical antipsychotics. The older typical antipsychotics are primarily dopamine antagonists.
Iloperidone has been shown to act as an antagonist at all tested receptors. It exhibits high (nM) affinity to serotonin 5HT2A (Ki value of 5.6 nM), dopamine D2 (6.3 nM) and D3 (7.1 nM) and noradrenaline α1 receptors (0.36 nM), moderate affinity for dopamine D4 (25 nM), serotonin 5HT6 (43 nM), 5HT7 (22 nM), and low affinity for the serotonin 5HT1A (168 nM), dopamine D1 and histamine H1 receptors. In addition, pharmacogenomic studies identified single nucleotide polymorphisms associated with an enhanced response to iloperidone during acute treatment of schizophrenia.
Iloperidone performed well against a prepulse inhibition (PPI) experiment, which was designed to gauge the extent of sensory gating in rats, a process disrupted in schizophrenia. Prepulse inhibition is the reduction in the amount of startle the subject gives when presented with a non-startling stimulus. Those exhibiting high levels of psychosis present a deficit in PPI. Psychosis induced using PCP, apomorphine, and cirazoline, were all prevented with the concurrent administration of iloperidone. The PPI deficit normally incurred by each psychotic drug was significantly diminished by the co administration of iloperidone. The results of this experiment provided strong evidence for iloperidone’s merit as an effective treatment for psychotic disorders. Iloperidone has also been shown to reduce the effects of apomorphine induced climbing behavior in mice as well as the effects of head twitching induced by 5-HT in rats.
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