Product Code Database
Iloperidone, sold under the brand name Fanapt among others, is an atypical antipsychotic for the treatment of schizophrenia and bipolar I disorder.
The approved dose is 12–24 mg, not 5 mg. However, claims of better tolerance have been reported.
There is tentative evidence that discontinuation of antipsychotics can result in psychosis. It may also result in reoccurrence of the condition that is being treated. Rarely tardive dyskinesia can occur when the medication is stopped.
Iloperidone has been shown to act as an antagonist at all tested receptors except for 5-HT2A. It exhibits high (nM) affinity to serotonin 5-HT2A (Ki value of 5.6 nM) where it acts as a inverse agonist. Antagonism occurs at all other receptors following dopamine D2 (6.3 nM) and D3 (7.1 nM) and α1-adrenergic receptors (0.36 nM), moderate affinity for dopamine D4 (25 nM), serotonin 5-HT6 (43 nM), 5-HT7 (22 nM), and low affinity for the serotonin 5-HT1A (168 nM), dopamine D1, and histamine H1 receptors. In addition, Pharmacogenomics studies identified single nucleotide polymorphisms associated with an enhanced response to iloperidone during acute treatment of schizophrenia.
Iloperidone was approved by the FDA for the treatment of schizophrenia in the United States on May 6, 2009. and for treating bipolar I disorder in April 2024.
Pharmacology
Iloperidone exerts its effects by 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.
(2025). 9780071769396, McGraw-Hill Medical. ISBN 9780071769396
History
Hoechst AG made initial inquiries into the drug; however, in May 1996, they discontinued research, and in June 1997 gave research rights to Titan Pharmaceuticals. Titan then handed over worldwide development, manufacturing and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals announced that the Phase III development rights have been acquired by Vanda Pharmaceuticals. The original launch date was scheduled for 2002. On November 27, 2007, Vanda Pharmaceuticals announced that the U.S. Food and Drug Administration (FDA) had accepted their New Drug Application for iloperidone, confirming the application is ready for FDA review and approval. On July 28, 2008, the FDA issued a not-approvable letter to Vanda Pharmaceuticals concerning the drug, stating that further trials are required before a decision can be made concerning marketed usage of iloperidone.
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