Pharmacokinetics and Tolerability Study of Risperidone ISM® in Schizophrenia

NCT02086786 | Completed Phase 2 Results

• 1 other identifier: ROV-RISP-2011-02
• Study Type: interventional
• Target: 70
• Locations: 1 country
• Sites: 1

Brief Summary

To characterize the pharmacokinetics (PK) of the injectable intramuscular (IM) long-acting formulation (in situ microparticle, ISM) of risperidone over four IM injections in the gluteal and deltoid muscle at 28-day intervals and at one dose strength (75 mg) in patients with schizophrenia.

Conditions

Schizophrenia

Outcome Measures

Primary Outcomes (8)

• Peak Plasma Concentration (Cmax) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• Trough Plasma Concentration (Cmin) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• Area Under the Curve to the Last Quantified Concentration (AUClast) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• Area Under the Curve Extrapolated to Infinity (AUC∞) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• AUCτ for Active Moiety

  AUCτ is the area under the curve over the dosing interval (τ), where the dosing interval is 28 days

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• Time to Peak Concentration (Tmax) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• Terminal Half-life (t1/2) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

• PTF for Active Moiety

  Peak to Trough Fluctuation ratio for the Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

Secondary Outcomes (1)

• Accumulation Ratio (RA) for Active Moiety

  Dose 1, 2 and 3: Pre-dose; at 2, 8, 12, 24 and 48 hours post-dose; 5, 7, 10, 14, 18, and 21 days post-dose. Dose 4: Pre dose; at 2, 8, 12, 24, and 48 hours post-dose; at 5, 7, 10, 14, 18, 21, 25, 28, 32, 37, 42, 60, 75, 90, 105, and 120 days post-dose.

Other Outcomes (1)

• Positive and Negative Syndrome Scale (PANSS) Total Score

  Baseline, Days 5, 7, 10, 14, 18, and 21 post Dose 1; Dose 2, 3 and 4 post dose; Days 5, 7, 10, 14, 18, and 21 post Dose 2, 3, and 4; Days 25, 28, 32, 37, 42, 60, 75, 90, and 105 post Dose 4; Day 120 post Dose 4 or early termination.

Study Arms (2)

Gluteus (Risperidone ISM)

EXPERIMENTAL

Risperidone ISM (75 mg) injection in the gluteal muscle at 28-day intervals

Drug: Risperidone ISM

Deltoid (Risperdione ISM)

EXPERIMENTAL

Risperidone ISM (75 mg) injection in the deltoid muscle at 28-day intervals

Drug: Risperidone ISM

Interventions

Risperidone ISM DRUG

Four doses of 75 mg of Risperidone ISM as intramuscular (IM) injection into the deltoid muscle at 28-day intervals. Four doses of 75 mg of Risperidone ISM as intramuscular injections into the gluteal muscle at 28-day intervals.

Also known as: No other names

Deltoid (Risperdione ISM); Gluteus (Risperidone ISM)

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.
• Current diagnosis of schizophrenia, according to Diagnostic and Statistical Manual
• Body mass index (BMI) ≥17 kg/m2 but ≤35 kg/m2.
• Medically stable over the last month, and psychiatrically stable
• On oral stable dosage of risperidone ≥4 mg daily as maintenance therapy.
• Total score ≤70 on the Positive and Negative Syndrome Scale.
• Using a medically accepted contraceptive method
• Agrees to washout all prohibited medications prior to baseline (day -1)

You may not qualify if:

• Informed consent obtained from a third party.
• Prisoners or patients who are compulsorily detained.
• Females who are breast-feeding and/or who have a positive pregnancy test.
• Presence of an uncontrolled, unstable clinically significant medical condition.
• Positive serology for Hepatitis B, Hepatitis C or anti-HIV 1 and 2 at screening.
• History of neuroleptic malignant syndrome.
• Current or past history of tardive dyskinesia.
• Positive urine drug or alcohol screen finding.
• Risk of committing self-harm or harm based on Columbia Suicidal Rating Scale.
• Taking more than one antidepressant.
• Use of depot antipsychotics within the last three months.
• Use of strong or moderate cytochrome P450 isoenzyme 3A4inducers
• Use of electroconvulsive therapy (ECT) within the last three months.
• Receipt of any investigational drugs within the last three months.
• Known or suspected allergy or hypersensitivity to risperidone

Sponsors & Collaborators

• Rovi Pharmaceuticals Laboratories: lead

Study Sites (1)

St Louis Clinical Trials, LC

St Louis, Missouri, 63141, United States

Location

MeSH Terms

Conditions

Schizophrenia

Condition Hierarchy (Ancestors)

Schizophrenia Spectrum and Other Psychotic Disorders; Mental Disorders

Results Point of Contact

• Title: Jordi Llaudó Garín ( Clinical Development Manager)
• Organization: Rovi S.A. Laboratorios Farmacéuticos

jllaudo@rovi.es

+34913756230

Study Officials

• Jordi Llaudó, M.D

  Rovi Laboratorios Farmacéuticos

  STUDY CHAIR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 2
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 10, 2014
• First Posted: March 13, 2014
• Study Start: March 1, 2014
• Primary Completion: March 1, 2015
• Study Completion: March 1, 2015
• Last Updated: July 13, 2017
• Results First Posted: July 13, 2017

Record last verified: 2015-05

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)