Pharmacokinetic Evaluation of Intranasal Nalmefene Using Three Dosing Regimens

NCT05219669 | Completed Phase 1 Results FDA Drug

• 1 other identifier: OPNT003-PK-002
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

This study is to compare the pharmacokinetics (how the body absorbs, breaks down and eliminates drug from your body) of nalmefene when given as a single dose intranasally (IN;into the nose), as a single dose in each nostril and as two doses in one nostrils; and to evaluate the safety and tolerability of nalmefene IN.

Conditions

Opioid Overdose

Keywords

Pharmacokinetics

Outcome Measures

Primary Outcomes (4)

• Maximum Plasma Concentration (Cmax)

  Maximum concentration of plasma nalmefene comparing 1 dose of IN in one nostril to 2 doses of IN in 1 nostril to 1 dose of IN in each nostril

  48 hours

• Time to Maximum Plasma Concentration (Tmax)

  Time to maximum concentration of plasma nalmefene comparing 1 dose of IN in one nostril to 2 doses of IN in 1 nostril to 1 dose of IN in each nostril

  48 hours

• Area Under the Curve (AUC)

  Area under the curve of plasma nalmefene comparing 1 dose of IN in one nostril to 2 doses of IN in 1 nostril to 1 dose of IN in each nostril

  48 hours

• Half-life (t1/2)

  Half life of plasma nalmefene comparing 1 dose of IN in one nostril to 2 doses of IN in 1 nostril to 1 dose of IN in each nostril

  48 hours

Study Arms (3)

Intranasal Nalmefene 1 Spray in 1 Nostril

EXPERIMENTAL

3 mg IN Nalmefene Hydrochloride dose (one 0.1 mL spray of a 30 mg/mL solution in one nostril)

Drug: Nalmefene Hydrochloride

Intranasal Nalmefene 2 Sprays in 1 Nostril

EXPERIMENTAL

6 mg IN Nalmefene Hydrochloride dose (two 0.1 mL sprays of a 30 mg/mL solution in one nostril)

Drug: Nalmefene Hydrochloride

Intranasal Nalmefene 1 Spray in Each Nostril

EXPERIMENTAL

6 mg IN Nalmefene Hydrochloride dose (one 0.1 mL spray of a 30 mg/mL solution in each nostril)

Drug: Nalmefene Hydrochloride

Interventions

Nalmefene Hydrochloride DRUG

30 mg/mL solution

Intranasal Nalmefene 1 Spray in 1 Nostril; Intranasal Nalmefene 1 Spray in Each Nostril; Intranasal Nalmefene 2 Sprays in 1 Nostril

Eligibility Criteria

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

You may qualify if:

• Male or female aged 18 to 55 years inclusive
• BMI ranging from 18 to 30 kg/m2, inclusive
• Adequate venous access
• Subjects must be non-smokers
• On screening and admission, the following standards had to be met before dosing and were permitted to be repeated once:
• Systolic blood pressure: 140 mmHg or less and equal to or greater than 90 mmHg
• Diastolic blood pressure: 90 mmHg or less and equal to or greater than 55 mmHg
• Heart rate: 100 beats per minute (bpm) or less and equal to or greater than 40 bpm
• Respiratory rate: 20 respirations per minute (rpm) or less and equal to or greater than 8 rpm

You may not qualify if:

• History of clinically significant disease
• Significant trauma injury, major surgery, open biopsy within 30 days prior to screening
• Following an abnormal diet 4 weeks prior to screening
• Use of prescribed or over the counter medications, dietary supplements, herbal products, vitamins or opioid analgesics 14 days before intervention and throughout the study
• Use of enzyme altering drugs 30 days before intervention or during the study
• Use of nasal products 28 days before intervention and throughout the study
• Experimental agents used at least 8 weeks prior to initial dosing for a period equivalent to 5 half-lives of the agent (whichever was longer).
• Positive urine drug test for alcohol, opioids, cocaine, methamphetamine, benzodiazepines, tetrahydrocannabinol (THC), barbiturates, or methadone at screening or admission.
• Previous or current opioid, alcohol, or other drug dependence (excluding nicotine and caffeine)
• Positive urine screen for cotinine (smoking and the use of tobacco products were not permitted for 4 weeks prior to the first dose of study drug and throughout the duration of the study).
• An ECG QTcF interval \>450 msec for males and \> or equal to 470 msec for females.
• Clinically significant concurrent medical conditions
• Donated or received blood 30 days before intervention
• Women who are pregnant or breastfeeding at screening and prior to each administration of study drug
• Women of childbearing potential unless surgically sterile or use effective contraception

Sponsors & Collaborators

• Opiant Pharmaceuticals Inc: lead

Study Sites (1)

WorldWide Clinical Trials

San Antonio, Texas, 78217, United States

Location

Related Publications (1)

• Crystal R, Ellison M, Purdon C, Skolnick P. Pharmacokinetic Properties of an FDA-approved Intranasal Nalmefene Formulation for the Treatment of Opioid Overdose. Clin Pharmacol Drug Dev. 2024 Jan;13(1):58-69. doi: 10.1002/cpdd.1312. Epub 2023 Jul 27.

  PMID: 37496452 DERIVED

MeSH Terms

Conditions

Opiate Overdose

Interventions

nalmefene

Condition Hierarchy (Ancestors)

Drug Overdose; Prescription Drug Misuse; Drug Misuse; Substance-Related Disorders; Chemically-Induced Disorders; Opioid-Related Disorders; Narcotic-Related Disorders; Mental Disorders

Results Point of Contact

• Title: Clinical Director
• Organization: Opiant Pharmaceuticals

PatientSafetyNA@Indivior.com

18043791090

Study Officials

• Ingela Danielsson, MD

  Worldwide Clinical Trials

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: No

Study Design

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

Study Record Dates

• First Submitted: January 21, 2022
• First Posted: February 2, 2022
• Study Start: September 1, 2021
• Primary Completion: November 19, 2021
• Study Completion: November 22, 2021
• Last Updated: August 5, 2024
• Results First Posted: August 5, 2024

Record last verified: 2024-02

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)