Evaluate Pharmacokinetics, Safety, and Tolerability of AX251 LAI in Patients With Schizophrenia

An Open-label, Multicenter Study to Determine the Pharmacokinetics, Safety, and Tolerability of AX251 Long-Acting Injectable (LAI) Administered as a Single Dose in Patients With Schizophrenia

Status

Recruiting

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT07484204

Enrollment

Registered

2026-03-20

Start date

2026-09-14

Completion date

2028-07-01

Last updated

2026-09-16

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Schizophrenia

Keywords

AX251

Brief summary

The purpose of this study is to assess the pharmacokinetics (PK), safety, and tolerability of AX251 long-acting injectable (LAI) administered as a single dose in patients with schizophrenia. The study will include sequential dose-escalation cohorts to evaluate different dose levels of AX251 LAI.

Interventions

DRUGAX251 LAI 45 mg

Cariprazine 45 mg

DRUGAX251 LAI 90 mg

Cariprazine 90 mg

DRUGAX251 LAI 135 mg

Cariprazine 135 mg

DRUGAX251 LAI 180 mg

Cariprazine 180 mg

Study design

Allocation

NON_RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 65 Years

Healthy volunteers

Inclusion criteria

* Male or female subjects aged 18 to 65 years (inclusive). * clinical diagnosis of schizophrenia per the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition, Text Revision (DSM-5-TR) (or later) criteria, at screening. * Body Mass Index (BMI) 18.5-35.0 kg/m² at screening. * Clinical Global Impression-Severity (CGI-S) score ≤4 at screening. * Positive and Negative Syndrome Scale (PANSS) total score ≤75 at screening. * Clinically stable schizophrenia on current antipsychotic medication other than cariprazine for at least 3 months prior to screening. * Subjects must not be taking more than two antipsychotic medications. * Able to remain at the study site for 7 days following AX251 LAI injection. * Judged by the investigator to be physically and mentally able to participate in the study based on clinical evaluation, physical examination, electrocardiogram (ECG), and laboratory assessments. * Willing and able to comply with study procedures. * Agrees to use protocol-defined contraception during the study. * Previous tolerability to oral cariprazine (1.5-6 mg) or willingness to undergo a short oral tolerability test (2-7 days) followed by washout before study drug administration.

Exclusion criteria

* Diagnosis of psychiatric disorders other than schizophrenia according to DSM-5-TR (e.g., schizoaffective disorder, major depressive disorder, bipolar disorder, generalized anxiety disorder, obsessive-compulsive disorder, post-traumatic stress disorder, dementia, mild neurocognitive disorder, or personality disorders), except caffeine- or tobacco-related disorders. * Substance use disorder (including alcohol or benzodiazepines) within 180 days prior to screening, excluding caffeine and tobacco. * History of neuroleptic malignant syndrome, seizure disorder, or clinically significant tardive dyskinesia, akathisia, or extrapyramidal symptoms. * Clinically significant cardiovascular, hematologic, metabolic, hepatic, renal, immunologic, or neurological disease that may interfere with study participation. * Severe hepatic impairment (Child-Pugh Class C) at screening. * Uncontrolled hypertension. * Clinically significant electrocardiogram abnormalities at screening. * Severe renal impairment (estimated glomerular filtration rate \<30 mL/min). * History of syncope or significant orthostatic hypotension at screening. * Failure to complete required washout period (≥5 half-lives) for prohibited medications before administration of AX251 LAI. * Current treatment with other antipsychotic long-acting injectable (LAI) therapies. * Electroconvulsive therapy within 60 days prior to screening. * Acute psychosis posing imminent risk to self or others. * Acute relapse of schizophrenia at screening.

Design outcomes

Primary

Measure	Time frame	Description
Pharmacokinetic Parameter	Day 1 pre-dose and 1, 2, 3, 4, 8, 12, and 24 hours post-dose. Days 3, 5, 7, 14, 21, 28, 42, 56, and 70	Maximum observed serum concentration of cariprazine and its metabolites desmethyl-cariprazine (DCAR) and didesmethyl-cariprazine (DDCAR) following a single dose of AX251 long-acting injectable (LAI).

Secondary

Measure	Time frame	Description
Safety: Incidence of Adverse Events (AEs) and Serious Adverse Events (SAEs)	Baseline to Day 70	Number and proportion of participants experiencing treatment-emergent adverse events and serious adverse events during the study.

Countries

India

Contacts

CONTACTMico Hsu

mico_hsu@anxo.com.tw886-5716223

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Sep 17, 2026