Pharmacokinetics, Safety and Tolerability of Different Formulations and Dose Strengths of Quarterly Risperidone (QUAR) in Patients With Schizophrenia

NCT06276361 | Completed Phase 1

• 1 other identifier: ROV-QUAR-2023-01
• Study Type: interventional
• Target: 58
• Locations: 1 country
• Sites: 1

Brief Summary

This is a single ascending dose phase 1 study to evaluate the pharmacokinetics (PK), safety, and tolerability of a single intramuscular (IM) injection of quarterly Risperidone (QUAR) for different formulations and dose strengths in participants with schizophrenia.

Conditions

Schizophrenia

Outcome Measures

Primary Outcomes (11)

• λz

  Terminal elimination rate constant

  Following Oral and QUAR administration until day 17 or 196 respectively

• t1/2

  Terminal elimination half-life

  Following Oral and QUAR administration until day 17 or 196 respectively

• Tmax

  Time to peak concentration

  Following Oral and QUAR administration until day 17 or 196 respectively

• Cmax

  Peak plasma concentration

  Following Oral and QUAR administration until day 17 or 196 respectively

• Cmin

  Minimum plasma concentration

  Following Oral and QUAR administration until day 17 or 196 respectively

• Clast

  Last observed plasma concentration

  Following Oral and QUAR administration until day 17 or 196 respectively

• AUC0-t

  Area under the curve

  Following Oral and QUAR administration until day 17 or 196 respectively

• AUCinf

  Area under the curve

  Following QUAR administration until day 196

• AUCextrap

  Area under the curve

  Following QUAR administration until day 196

• Vd/F

  Apparent volume of distribution

  Following Oral and QUAR administration until day 17 or 196 respectively

• Cl/F

  Apparent total body clearance

  Following Oral and QUAR administration until day 17 or 196 respectively

Study Arms (4)

Cohort 1/2

EXPERIMENTAL

Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 1 dose.

Drug: Oral risperidone; QUAR F1/2, Dose 1 - Gluteal

Cohort 1a/2a

EXPERIMENTAL

Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 2 dose.

Drug: Oral risperidone; QUAR F1/2, Dose 2 - Gluteal

Cohort 1b//2b

EXPERIMENTAL

Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 3 dose.

Drug: Oral risperidone; QUAR F1/2, Dose 3 - Gluteal

Cohort 1c/2c

EXPERIMENTAL

Patient will recieve oral risperidone for one week followed by a single IM injection of Risperidone QUAR out of two possible formulations (F1/F2) with a level 3 dose.

Drug: Oral risperidone; QUAR F1/2, Dose 3 - Deltoids

Interventions

Oral risperidone; QUAR F1/2, Dose 1 - Gluteal DRUG

Dose level 1

Cohort 1/2

Oral risperidone; QUAR F1/2, Dose 2 - Gluteal DRUG

Dose level 2

Cohort 1a/2a

Oral risperidone; QUAR F1/2, Dose 3 - Gluteal DRUG

Dose level 3

Cohort 1b//2b

Oral risperidone; QUAR F1/2, Dose 3 - Deltoids DRUG

Dose level 3

Cohort 1c/2c

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Capable of providing informed consent.
• Male or female aged ≥ 18 years to \< 65 years with BMI ≥17.0 to ≤35.0 kg/m2
• Current diagnosis of schizophrenia, according to the Diagnostic and DSM-5 criteria.
• Medically stable over the last month, and psychiatrically stable without significant symptom exacerbation over the last three months based on the investigator's judgment
• currently taking oral risperidone as maintenance therapy
• Score of ≤ 4 (moderately ill at most) on the Clinical Global Impression - Severity of Illness (CGI-S)
• If a sexually active female of childbearing potential, using a medically accepted method of birth control.

You may not qualify if:

• Presence of an uncontrolled, unstable, clinically significant medical condition that in the opinion of the investigator could interfere with the interpretation of safety and PK evaluations
• If female, a positive serum pregnancy test, or planning to become pregnant between signing informed consent and 1 month after the last dose of study drug or is breastfeeding a child.
• History of neuroleptic malignant syndrome and current or past history of clinically significant tardive dyskinesia.
• The participant has a primary diagnosis other than schizophrenia diagnosis that is primarily responsible for current symptoms and functional impairment
• Positive test result for drugs of abuse or alcohol unless the positive finding can be accounted for by documented prescription use.
• In the investigator's opinion, at imminent risk of committing self-harm or harm to others.
• Unwilling to discontinue any of the prohibited medications prior to the baseline visit or unable to safely washout such medication without significant destabilization or increased risk of self-harm (suicide).
• Receipt study drug in another investigational study in the last 90 days.
• Current participation in any other clinical trial.

Sponsors & Collaborators

• Rovi Pharmaceuticals Laboratories: lead

Study Sites (1)

Investigational Site

Amman, Jordan

Location

MeSH Terms

Conditions

Schizophrenia

Interventions

Risperidone

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Intervention Hierarchy (Ancestors)

Pyrimidinones; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 16, 2024
• First Posted: February 26, 2024
• Study Start: September 26, 2023
• Primary Completion: July 7, 2025
• Study Completion: July 7, 2025
• Last Updated: September 8, 2025

Record last verified: 2025-09

Locations

JO (1)