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

Trial Summary

What is the purpose of this trial?

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 after a single intramuscular injection in patients with stale schizophrenia or schizoaffective disorder.

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.

What data supports the effectiveness of the drug Lumateperone for treating schizophrenia?

Lumateperone has been shown to be effective in treating schizophrenia through its unique action on serotonin, dopamine, and glutamate, which helps improve various symptoms of the condition. Clinical trials have demonstrated its efficacy and favorable tolerability in patients with schizophrenia. ^{1 2 3 4 5}

Is lumateperone safe for humans?

Lumateperone has been shown to be generally safe and well-tolerated in studies for schizophrenia, with no significant changes in vital signs or lab values, and a lower risk of movement disorders compared to other antipsychotic drugs. ^{1 2 4 5 6}

How is the drug Lumateperone unique in treating schizophrenia?

Lumateperone is unique because it simultaneously modulates serotonin, dopamine, and glutamate neurotransmission, which may help with a wide range of schizophrenia symptoms, including positive, negative, cognitive, and social symptoms. It also has a favorable safety profile, with fewer side effects like movement disorders or hormonal changes compared to other antipsychotics. ^{2 3 4 5 7}

Eligibility Criteria

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.

I am between 18 and 55 years old with a diagnosis of schizophrenia or schizoaffective disorder.

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

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

Treatment Details

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.

Participant Groups

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+

Findings from Research

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]

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 (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 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]

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]

References

1. Netherlands pubmed.ncbi.nlm.nih.gov

Safety and tolerability of lumateperone 42 mg: An open-label antipsychotic switch study in outpatients with stable schizophrenia. [2021]

2. United States pubmed.ncbi.nlm.nih.gov

Lumateperone: New Drug or Same Old Drug With a New Dress? [2021]

3. United States pubmed.ncbi.nlm.nih.gov

Lumateperone for the Treatment of Adults With Schizophrenia: a Systematic Review. [2022]

4. England pubmed.ncbi.nlm.nih.gov

An evaluation of lumateperone tosylate for the treatment of schizophrenia. [2020]

5. New Zealand pubmed.ncbi.nlm.nih.gov

Lumateperone: First Approval. [2021]

6. England pubmed.ncbi.nlm.nih.gov

Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia. [2020]

7. United Arab Emirates pubmed.ncbi.nlm.nih.gov

Evidence on the New Drug Lumateperone (ITI-007) for Psychiatric and Neurological Disorders. [2021]