New Drugs For Schizophrenia! Intra-cellular Therapies Company, Caplyta(lumateperone), Was Approved By U.S. FDA

- Jan 03, 2020-

Intra-Cellular Therapies (ICT) is a biopharmaceutical company focused on developing innovative therapies for diseases of the central nervous system (CNS). Recently, the company announced that the US Food and Drug Administration (FDA) has approved Caplyta (lumateperone) for the treatment of adult patients with schizophrenia. The company expects to launch Caplyta to the market by the end of the first quarter of 2020.


In terms of medication, the recommended dose of Caplyta is 42mg, once daily, taken with food and not requiring a dose titration. It should be noted that the label of Caplyta's medication contains a black-boxed warning indicating that patients with dementia-related psychosis are at increased risk of death when treated with antipsychotics. Caplyta is not approved for the treatment of dementia-related psychiatric patients.


The efficacy of Caplyta 42mg was demonstrated in two placebo-controlled trials with statistically significant differences in the overall score of the primary endpoint, the positive and negative symptom scale (PANSS).The most common adverse effects of the recommended dose of Caplyta compared to placebo (≥5% and twice as common as placebo) included drowsiness/sedation (24% vs 10%) and dry mouth (6% vs 2%).


In the pooled data from the short-term studies, weight gain, fasting glucose, triglycerides, and total cholesterol in the Caplyta and placebo groups were similar to the mean changes in baseline levels.The incidence of extrapylic symptoms was 6.7% in the Caplyta group and 6.3% in the placebo group.

 Caplyta is lumateperone

ICT chairman and chief executive Dr Sharon Mates said: "we are confident that Caplyta will provide healthcare providers with a new, safe and effective treatment option that will help millions of adults with schizophrenia. The approval marks the culmination of years of scientific research. We are particularly grateful to patients, their carers and the healthcare professionals who have contributed to the development of Caplyta."


Schizophrenia is a kind of serious mental illness that affects about 2.4 million American adults schizophrenia is the characteristics of various clinical manifestations of acute psychiatric symptoms, including hallucinations and delusions, often need to be hospitalized for the treatment of this disease is chronic and lifelong, often accompanied by depression and social function and cognitive abilities gradually deteriorated schizophrenia patients often due to side effects such as weight gain and movement disorders and stop treatment.


The active pharmaceutical ingredient of Caplyta is lumateperone, a first-in-class small-molecule drug that can selectively and simultaneously regulate serotonin, dopamine and glutamate, three neurotransmitter pathways involved in serious diseases. Unlike existing schizophrenia drugs, lumateperone is a dopamine receptor phosphate protein modulator (DPPM) that ACTS as a presynaptic partial agonist and a postsynaptic antagonist on the D2 receptor.


This mechanism, along with potential interactions with 5-ht2a receptors, serotonin transporters, and D1 receptors, as well as indirect glutamate regulation, may contribute to lumateperone's efficacy across a range of psychiatric symptoms, with improved psychosocial function and good tolerance. The compound has the potential to benefit patients with a range of neuropsychiatric disorders and neurodegenerative diseases.


lumateperone structural formula

lumateperone structural formula

In the United States, the FDA granted lumateperone fast-track status for treating schizophrenia in November 2017.In addition to schizophrenia, ICT is also developing lumateperone for the treatment of other psychiatric disorders, including behavioral disorders in dementia patients, alzheimer's disease, depression, and other neuropsychiatric and neurological disorders.


In July, lumateperone was the top-line outcome of two phase III clinical studies (Study 401, Study 404) using single drug therapy for bipolar I disorder or bipolar ii-related major depression. Data showed that lumateperone 42mg reached the primary end point for improving depression (p < 0.001) and the key secondary end point for improving depression severity (p < 0.001) in the 404 study compared to the placebo group. However, in the 401 study, both doses of lumateperone (42mg and 28mg) did not reach the primary end point because of the high clinical response in the placebo group. Lumateperone showed good safety and tolerability in 2 studies.