Iloperidone

Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia.

Availability

It was approved by the U.S. Food and Drug Administration (FDA) for use in the United States on May 6, 2009.

Pharmacology

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 5HT_2A (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 5HT_1A (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.