Bioavailability Study of Naloxone 5 Milligrams (mg) Intramuscular (IM) Autoinjector

NCT05264493 | Completed Phase 1 FDA Drug

• 1 other identifier: C2431001
• Study Type: interventional
• Target: 13
• Locations: 1 country
• Sites: 1

Brief Summary

To compare the plasma concentration (bioavailability) and safety of a single naloxone 5 mg autoinjector intramuscular (IM) injection to a single 2 mg IM injection (an approved safe dose) and to a single 2 mg bolus intravenous (IV) injection (an approved safe dose)

Conditions

Healthy Volunteers

Keywords

naloxone; autoinjector; intramuscular; high dose; 5 mg; healthy volunteers; safety; cross-over study; pharmacokinetics; 3 treatment arms

Outcome Measures

Primary Outcomes (2)

• Maximum observed plasma naloxone concentration (Cmax) of a single 5 mg IM autoinjector injection compared to a 2 mg IM injection

  Comparison of bioavailability

  predose, 2.5, 5, 10, 15, 30, 45, 60, 90, 120, 180, 240, 360, 480, and 1440 minutes after dose

• Area under the naloxone concentration versus time curve (AUC) from time zero to the last collection time (AUClast) of a single 5 mg IM autoinjector injection compared to a 2 mg IM injection

  Comparison of bioavailability

  predose, 2.5, 5, 10, 15, 30, 45, 60, 90, 120, 180, 240, 360, 480, and 1440 minutes after dose

Secondary Outcomes (11)

• AUC from time zero to 2.5 minutes (AUC0-2.5)

  predose and 2.5 minutes after dose

• AUC from time zero to 5 minutes (AUC0-5)

  predose, 2.5 and 5 minutes after dose

• AUC from time zero to 15 minutes (AUC0-15)

  predose, 2.5, 5, 10 and 15 minutes after dose

• AUC from time zero to 30 minutes (AUC0-30)

  predose, 2.5, 5, 10, 15, and 30 minutes after dose

• AUC from time zero extrapolated to infinity (AUCinf) [if data permit]

  predose, 2.5, 5, 10, 15, 30, 60,90, 120, 180, 240, 360, 480, 1440 minutes after dose

Study Arms (3)

naloxone 5 mg IM autoinjector

EXPERIMENTAL

participants will receive in random order, a single naloxone 5 mg IM autoinjector injection into the lateral thigh

Drug: NaxRedy ™

naloxone 2 mg IM

ACTIVE COMPARATOR

participants will receive in random order, a single naloxone 2 mg IM injection into the gluteus muscle

Drug: Naloxone Hydrochloride Injection, USP

naloxone 2mg bolus IV

ACTIVE COMPARATOR

participants will receive in random order, a single naloxone 2 mg bolus IV injection

Drug: Naloxone Hydrochloride Injection, USP

Interventions

NaxRedy ™ DRUG

5 mg (5 mg/0.5 mL) IM autoinjector injection into lateral thigh

naloxone 5 mg IM autoinjector

Naloxone Hydrochloride Injection, USP DRUG

2 mg IM (2mg/2 mL) injection into gluteal muscle

naloxone 2 mg IM

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants are eligible to be included in the study only if all of the following criteria apply:
• Age and Sex:
• Healthy male and/or female participants of non-childbearing potential, who, at the time of screening, are between the ages of 18 and 55 years, inclusive.
• Refer to protocol for reproductive criteria for male and female participants.
• Type of Participant and Disease Characteristics:
• Male and female participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, vital signs, 12-lead ECG, and/or clinical laboratory tests.
• Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures.
• Weight:
• BMI of 17.5 to 30.5 kg/m2; and a total body weight \> 50 kg (110 lb).
• Informed Consent:
• \. Capable of giving signed informed consent as described in Appendix 1, which includes compliance with the requirements and restrictions listed in the ICD and in this protocol.

You may not qualify if:

• Participants are excluded from the study if any of the following criteria apply:
• Medical Conditions:
• Other medical or psychiatric condition including recent (within the past year) or active suicidal ideation/behavior or laboratory abnormality that may increase the risk of study participation or, in the investigator's judgment, make the participant inappropriate for the study.
• Current or past diagnosis of any type of drug dependence within the past year will not be eligible to participate. History of alcohol abuse, dependence or binge drinking and/or any other illicit drug use within 6 months of screening. Binge drinking is hours. As a general rule, alcohol intake should not exceed 14 units per week (1 unit = 8 ounces (240 mL) beer, 1 ounce (30 mL) of 40% spirit or 3 ounces (90 mL) of wine).
• If fever is present within 7 days of admission or screening.
• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
• History of HIV infection, hepatitis B, or hepatitis C, positive testing for HIV, HBsAg, or HCVAb. Hepatitis B vaccination is allowed.
• Other medical or psychiatric condition including recent (within the past year) or active suicidal ideation/behavior or laboratory abnormality that may increase the risk of study participation or, in the investigator's judgment, make the participant inappropriate for the study.
• Prior/Concomitant Therapy:
• Use of prescription or nonprescription drugs and dietary and herbal supplements within 14 days or 5 half-lives (whichever is longer) prior to the first dose of study intervention. Prior/Concurrent Clinical Study Experience:
• Previous administration with an investigational drug within 30 days (or as determined by the local requirement) or 5 half-lives preceding the first dose of study intervention used in this study (whichever is longer).
• Diagnostic Assessments:
• A positive urine drug test.
• Has participated in, is currently participating in, or is seeking treatment for substance-and/or alcohol-related disorders (excluding nicotine and caffeine).
• Has a positive alcohol breathalyzer test at screening or upon admission to the study center of Treatment Period. Positive results may be repeated and/or participants re-scheduled at the investigator's discretions.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

New Haven Clinical Research Unit

New Haven, Connecticut, 06511, United States

Location

Related Links

• To obtain contact information for a study center near you, click here.

MeSH Terms

Interventions

Naloxone

Intervention Hierarchy (Ancestors)

Morphinans; Opiate Alkaloids; Alkaloids; Heterocyclic Compounds; Heterocyclic Compounds, Bridged-Ring; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Phenanthrenes; Polycyclic Aromatic Hydrocarbons; Polycyclic Compounds

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

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

Model Details: Williams Square Study Design with 6 sequences

Study Record Dates

• First Submitted: February 14, 2022
• First Posted: March 3, 2022
• Study Start: October 6, 2020
• Primary Completion: January 8, 2021
• Study Completion: January 8, 2021
• Last Updated: March 3, 2022

Record last verified: 2022-03

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)