Pharmacokinetic and Safety Study of Naltrexone Release From Subcutaneous BICX104 Pellets Compared to Vivitrol Injections

A Randomized, Open Label, Single Dose Pharmacokinetic and Safety Study of Implantable Long Acting 3-month Naltrexone Subcutaneous Pellets Compared to Naltrexone IM Injection (Vivitrol) in Healthy Volunteers

This is a Phase 1, 6-month, open-label, multi-center study in parallel groups of randomized healthy volunteers to evaluate the pharmacokinetics and safety of BICX104 implantable subcutaneous naltrexone pellets and Vivitrol intramuscular depot naltrexone injection.

Study Overview

• Status: Completed
• Conditions: Opioid-use Disorder
• Intervention / Treatment: Drug: BICX104; Drug: Vivitrol

• Study Type: Interventional
• Enrollment (Actual): 24
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • California
    • Tustin, California, United States, 92780
      • Orange County Research Center

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 50 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

1. Willing and able to provide informed consent.
2. Female or male subjects aged 18-50 years old.
3. Without current non-remitted DSM-5 (The Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition) - Substance Use Disorders diagnoses; subjects with a sustained remission diagnosis are not excluded.
4. In good health, as determined by the study physician, based on complete medical history, physical examination, vital signs measurement, ECG, and laboratory tests within normal ranges, to permit treatment.
5. Weight of 100-180 pounds, and a BMI of 18.5 to 30 kg/m2, inclusive.
6. Must agree to comply with all study requirements and be willing to complete entire study.
7. Females of childbearing potential and males willing to practice an effective method(s) of birth control for the duration of participation in the study (<1% failure rate per year).

Exclusion Criteria:

1. Is pregnant, is planning to become pregnant or breastfeed infants during the study.
2. Is currently treated with naltrexone or has had a naltrexone implant in the past 2 years or received Vivitrol treatment in the past year.
3. Clinically significant medical/psychological condition or abnormality at screening (i.e., physical examination, electrocardiogram [ECG], hematology or blood chemistry evaluation, or urinalysis findings), including any diagnosis of Hepatitis B, Hepatitis C or HIV infection.
4. Presence of opiates, cocaine, methamphetamine or other significant drugs of abuse in the urine (as determined by urine drug test).
5. Any active hepatitis or hepatic failure or dysfunction evidenced by the following: aspartate transaminase (AST) or alanine transaminase (ALT) higher than 1.5 times the upper limit of normal (1.5xULN), hyperbilirubinemia (bilirubin >10% above ULN), creatine phosphokinase (CPK) higher than 2.5xULN, prolonged prothrombin time (international normalized ratio ≥1.7), ascites, or esophageal variceal disease.
6. Manifestation of suicidal ideation, psychotic symptoms (including significant violent behavior), or psychiatric or neurological disorders that would compromise ability to complete the study.
7. Participation in a methadone program currently or within past 3 years, or 3 or more previous medically supervised detoxification treatments in past 3 years.
8. If a healthy volunteer fails one naloxone challenge, the subject will not be suitable for the study. The only exceptions will be made when a 'false positive' test result is received for the first test.
9. Intolerance and/or hypersensitivity to naltrexone, naloxone, or polylactide-co-polymers such as polylactide-co-glycolide (PLG).
10. Participation in a clinical trial within 30 days of screening.
11. Has a condition which requires or may require treatment with opioid based medication.
12. Is prone to skin rashes, irritation or has a chronic skin condition.
13. Alcohol Use Disorder diagnosis.
14. Has a predisposition to poor response to an implant site reaction, as judged by the study physician.
15. Has a history of keloid formation, connective tissue disease, e.g., scleroderma, or history of recurrent MRSA infections.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: BICX104; BICX104 is an eroding implantable pellet that contains 1 g naltrexone and 11 mg magnesium stearate that will be inserted subcutaneously. It will be administered once for 84 days.	Drug: BICX104; Erodable implantable pellet containing 1 g naltrexone and 11 mg magnesium stearate.
Active Comparator: Vivitrol; Vivitrol intramuscular injection containing 380 mg of naltrexone. Three consecutive doses will be administered once every 28 days for 84 days.	Drug: Vivitrol; Intramuscular injection containing 380 mg of naltrexone.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic parameter: Cmax.	Maximum observed mean plasma concentration [Cmax] of naltrexone and 6-beta-naltrexol.	140 Days
Pharmacokinetic parameter: Tmax.	Time to mean maximum observed drug concentration (Tmax) of naltrexone and 6-beta-naltrexol.	140 Days
Pharmacokinetic parameter: Css.	Changes in the mean observed steady state plasma concentration [Css] of naltrexone and 6-beta-naltrexol.	140 Days
Pharmacokinetic parameter: AUC	Area Under the Plasma Concentration Versus Time Curve (AUC) of naltrexone and 6-beta-naltrexol.	140 Days
Pharmacokinetic parameter: Tlast ≥ 1ng/ml naltrexone.	Time of Last Quantifiable Plasma Concentration (Tlast) of naltrexone greater than or equal to 1ng/ml.	140 Days
Pharmacokinetic parameter: Tlast.	Time of Last Quantifiable Plasma Concentration (Tlast) of naltrexone and 6-beta-naltrexol.	140 Days

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety Parameter: AEs	Incidence and severity of adverse events (AEs)	168 Days

Collaborators and Investigators

• Sponsor: BioCorRx Inc
• Collaborators: National Institute on Drug Abuse (NIDA); The HEAL Initiative (https://heal.nih.gov/)

Study record dates

Study Major Dates

• Study Start (Actual): June 17, 2022
• Primary Completion (Actual): February 22, 2023
• Study Completion (Actual): March 22, 2023

Study Registration Dates

• First Submitted: March 26, 2021
• First Submitted That Met QC Criteria: March 30, 2021
• First Posted (Actual): April 2, 2021

Study Record Updates

• Last Update Posted (Actual): August 16, 2023
• Last Update Submitted That Met QC Criteria: August 14, 2023
• Last Verified: March 1, 2023

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Mental Disorders; Chemically-Induced Disorders; Substance-Related Disorders; Narcotic-Related Disorders; Opioid-Related Disorders; Physiological Effects of Drugs; Peripheral Nervous System Agents; Sensory System Agents; Narcotic Antagonists; Alcohol Deterrents; Naltrexone
• Other Study ID Numbers: BioCorRx-21-01a; UG3DA047925 (U.S. NIH Grant/Contract)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No