Lumateperone for Schizophrenia

Recruiting at 3 trial locations

Overseen By ITI Clinical Trials

Age: 18 - 65

Sex: Any

Trial Phase: Phase 1

Sponsor: Intra-Cellular Therapies, Inc.

Disqualifiers: Other psychiatric conditions, Suicidal ideation, others

No Placebo Group All trial participants will receive the active study treatment (no placebo)

Approved in 1 Jurisdiction This treatment is already approved in other countries

Compensation: Varies

Number of Visits: 1

Duration: 2 weeks

72 Participants Needed

What You Need to Know Before You Apply

What is the purpose of this trial?

This trial tests a new long-acting injectable form of lumateperone, a medication for treating schizophrenia and schizoaffective disorder. Researchers aim to determine the safety of this new version and how the body processes it. Different groups will receive various versions of the treatment to identify the best option. This trial may suit individuals who have been stable with schizophrenia or schizoaffective disorder for at least three months without severe symptoms. As a Phase 1 trial, the research focuses on understanding how the treatment works in people, offering participants the opportunity to be among the first to receive this new form of medication.

Will I have to stop taking my current medications?

The trial information does not specify if you need to stop taking your current medications. It's best to discuss this with the study team or your doctor.

Is there any evidence suggesting that lumateperone long-acting injectable is likely to be safe for humans?

Research has shown that lumateperone is generally safe for humans. In past studies, participants using lumateperone long-acting injectable (LAI) forms reported few side effects, with many experiencing no major issues.

The FDA has already approved lumateperone for treating schizophrenia, indicating its general safety. Although this trial is in the early stages, FDA approval suggests it has undergone safety testing in similar treatments. However, new formulations can produce different effects.

Prospective trial participants should know that early-stage trials primarily focus on safety and treatment tolerance. Researchers closely monitor participants for any potential issues. ^{1 2 3 4 5}

Why do researchers think this study treatment might be promising?

Lumateperone is unique because it offers a long-acting injectable option for treating schizophrenia, which could mean fewer doses and improved patient compliance compared to daily oral medications. Unlike traditional antipsychotics that primarily target dopamine receptors, lumateperone works through a novel mechanism by modulating serotonin and glutamate pathways as well, potentially offering a broader therapeutic effect. Researchers are excited because this could lead to better management of symptoms with fewer side effects, addressing significant unmet needs in schizophrenia treatment.

What evidence suggests that lumateperone long-acting injectable could be an effective treatment for schizophrenia?

Research has shown that lumateperone, the investigational treatment in this trial, effectively treats symptoms of schizophrenia. It alleviates positive symptoms like hallucinations and negative symptoms like social withdrawal. Studies also indicate it improves thinking and memory problems. Long-term evidence found that lumateperone reduced the risk of relapse by 63% in adults with schizophrenia compared to those not taking it, suggesting it may help prevent symptoms from returning. Overall, lumateperone is considered effective for managing various aspects of schizophrenia. Participants in this trial will receive different formulations of lumateperone to further evaluate its effectiveness. ^{2 3 5 6 7}

Are You a Good Fit for This Trial?

This trial is for patients with stable schizophrenia or schizoaffective disorder. Specific eligibility details are not provided, but typically participants must meet certain health criteria and not be taking conflicting medications.

Inclusion Criteria

My mental health condition is considered mild to moderate.

I have been mentally stable and free from severe mental health episodes for at least 3 months.

My BMI is between 18 and 38, and I weigh at least 50 kg.

Exclusion Criteria

History of psychiatric condition other than schizophrenia that may be detrimental to participation in the study

Any suicidal ideation or attempt within specific timeframes, or current safety concerns based on C-SSRS

Clinically significant abnormality within 2 years of Screening that may place the patient at risk or interfere with study outcome variables

Timeline for a Trial Participant

Screening

Participants are screened for eligibility to participate in the trial

2-4 weeks

Treatment

Participants receive lumateperone 42 mg once daily for 5 days followed by a single intramuscular dose of lumateperone LAI formulation after a 5-day washout

2 weeks

1 visit (in-person) for IM dose

Follow-up

Participants are monitored for safety and effectiveness after treatment, with pharmacokinetic measurements taken up to Day 60

8 weeks

Multiple visits for PK measurements

What Are the Treatments Tested in This Trial?

Interventions

• Lumateperone Long-Acting Injectable

Trial Overview The study is testing the safety and how the body processes Lumateperone when given as a long-acting injectable (LAI). It's an open-label Phase 1b trial, meaning everyone knows they're getting the drug, and it's given once by injection.

How Is the Trial Designed?

Group I: Cohort 9 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> dose in Part B) of lumateperone LAI formulation (chosen from Part B) after a 5-day washout

Group II: Cohort 8 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> dose in Part B) of lumateperone LAI formulation (chosen from Part B) after a 5-day washout

Group III: Cohort 7 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Group IV: Cohort 6 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Group V: Cohort 5 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose (\> 100 mg) of lumateperone LAI formulation (chosen from Part A) after a 5-day washout

Group VI: Cohort 4 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-X5 after a 5-day washout

Group VII: Cohort 3 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-X2 after a 5-day washout

Group VIII: Cohort 2 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-E3 after a 5-day washout

Group IX: Cohort 1 Experimental Treatment 2 Interventions

Lumateperone 42 mg once daily for 5 days following by a single IM dose of lumateperone 100 mg LAI formulation X500-E2 after a 5-day washout

Lumateperone Long-Acting Injectable is already approved in United States for the following indications:

Approved in United States as Caplyta for:

• Schizophrenia
• Bipolar depression

Who Is Running the Clinical Trial?

Intra-Cellular Therapies, Inc.

Lead Sponsor

Trials

42

Recruited

10,700+

Published Research Related to This Trial

In a study of 301 outpatients with stable schizophrenia, lumateperone was found to be well tolerated, with only 45.5% experiencing treatment-emergent adverse events, most of which were mild or moderate, and a very low incidence of extrapyramidal symptoms (1.0%).

Patients switching to lumateperone showed significant improvements in metabolic parameters, such as reduced cholesterol and body weight, while maintaining stable schizophrenia symptoms, indicating its safety and efficacy compared to previous antipsychotic treatments.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Safety and tolerability of lumateperone 42 mg: An open-label antipsychotic switch study in outpatients with stable schizophrenia. Correll, CU., Vanover, KE., Davis, RE., et al.[2021]

In a study involving 10 patients with schizophrenia, lumateperone (ITI-007) demonstrated a mean dopamine D2 receptor occupancy of 39% after a 60 mg dose, which is lower than most traditional antipsychotics, potentially leading to fewer side effects.

Lumateperone was well-tolerated with no significant adverse effects, such as motor disturbances or increased prolactin levels, suggesting it may offer a safer treatment alternative for schizophrenia.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia. Vanover, KE., Davis, RE., Zhou, Y., et al.[2020]

Lumateperone (ITI-007) has a unique mechanism of action that targets multiple neurotransmitter systems, including serotonin, dopamine, and glutamate, making it a promising treatment for schizophrenia and potentially other psychiatric conditions.

It has shown a favorable safety profile, with no significant side effects like extrapyramidal symptoms or hyperprolactinemia, suggesting it could be a safer alternative to traditional antipsychotics.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Evidence on the New Drug Lumateperone (ITI-007) for Psychiatric and Neurological Disorders. Mazza, M., Marano, G., Traversi, G., et al.[2021]

Lumateperone (LUM) has been shown to significantly reduce the severity of schizophrenia symptoms compared to placebo, based on data from four clinical studies involving randomized controlled trials and an open-label trial.

LUM has a favorable safety and tolerability profile, exhibiting placebo-level rates of weight gain, metabolic changes, and extrapyramidal side effects, making it a strong candidate for first-line treatment in adults with schizophrenia.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Lumateperone for the Treatment of Adults With Schizophrenia: a Systematic Review. Jawad, MY., Alnefeesi, Y., Ceban, F., et al.[2022]

Lumateperone (Caplyta®) is a newly approved medication for schizophrenia that works by blocking serotonin 2A receptors and has a unique mechanism involving partial agonism at presynaptic dopamine receptors and modulation of glutamate receptors, which may help address symptoms of the disorder.

Clinical trials (Phase II and III) suggest that Lumateperone's novel mechanism could offer benefits in treating schizophrenia, although it shares similarities with existing second- and third-generation antipsychotics.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Lumateperone: New Drug or Same Old Drug With a New Dress? Limandri, BJ.[2021]

Lumateperone is a first-in-class investigational drug for schizophrenia that works by targeting multiple neurotransmitter systems, including serotonergic, glutamatergic, and dopaminergic pathways, which may help alleviate a wide range of symptoms associated with the disorder.

Clinical trials suggest that lumateperone has unique pharmacological properties that could significantly improve schizophrenia symptoms, and future studies are expected to provide more insights into its long-term efficacy and safety.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

An evaluation of lumateperone tosylate for the treatment of schizophrenia. Vyas, P., Hwang, BJ., Brašić, JR.[2020]

Lumateperone (Caplyta®) is a first-in-class medication that modulates serotonin, dopamine, and glutamate, making it a unique treatment option for schizophrenia and potentially other neuropsychiatric disorders.

Approved in December 2019 for schizophrenia in adults, lumateperone is also being studied for various conditions, including bipolar depression and Alzheimer's-related behavioral disorders, highlighting its broad therapeutic potential.

NCBI (Pubmed)

pubmed.ncbi.nlm.nih.gov

Lumateperone: First Approval. Blair, HA.[2021]

Citations

1. pmc.ncbi.nlm.nih.gov pmc.ncbi.nlm.nih.gov/articles/PMC10741391/

The Novel Antipsychotic Lumateperone (Iti-007) in the ... Lumateperone has demonstrated effectiveness in addressing positive, negative, and cognitive symptoms associated with schizophrenia.

2. jnj.com jnj.com/media-center/press-releases/supplemental-new-drug-application-submitted-to-u-s-fda-for-caplyta-lumateperone-with-data-demonstrating-significant-schizophrenia-relapse-prevention-compared-to-placebo

Supplemental new drug application submitted to U.S. FDA ... Submission is based on long-term Phase 3 data demonstrating 63 percent reduction in risk of relapse in adults with schizophrenia compared to ...

3. clinicaltrials.gov clinicaltrials.gov/study/NCT06627413?term=LUMATEPERONE&rank=1

Study Details | NCT06627413 | Safety, Tolerability, and ... Safety, Tolerability, and Pharmacokinetics of Lumateperone Long-Acting Injectable Formulations in Patients With Schizophrenia or Schizoaffective Disorder.

4. psychiatrist.com psychiatrist.com/jcp/lumateperone-adjunctive-therapy-major-depressive-disorder-randomized-double-blind-phase-3-trial/

Lumateperone as Adjunctive Therapy in Patients With ... With lumateperone 42 mg+ADT, MADRS response and remission rates at day 43 were significantly greater than those of placebo +ADT, with similar or ...

5. academic.oup.com academic.oup.com/ijnp/article/27/11/pyae052/7863712

Efficacy and safety of lumateperone for bipolar depression ... Lumateperone was efficacious in reducing depressive symptoms in bipolar depression (SMDs = −0.36, 95% CI: −.59 to −.13). In treating schizophrenia, lumateperone ...

6. clinicaltrials.gov clinicaltrials.gov/study/NCT04709224

Study Details | NCT04709224 | Pharmacokinetics, Safety, ... This is an open-label study to determine the pharmacokinetics, safety and tolerability of single ascending doses of lumateperone long-acting injectable ...

7. connect.careboxhealth.com connect.careboxhealth.com/en-US/trial/listing/537722

Safety, Tolerability, and Pharmacokinetics of Lumateperone ... Study ITI-007-037 is a Phase 1b, open-label study to evaluate the safety, tolerability, and PK of lumateperone long-acting injectable (LAI) formulations ...