Pharmacokinetic (PK) Evaluation of Nalmefene Formulations

Knoa Pharma LLC13 enrolled

Overview

This study is designed to characterize the PK of nalmefene following IV bolus and IM injections using nalmefene 0.5 mg (0.94% MgCl2) and IV bolus of 0.5 mg nalmefene hydrochloride injection in healthy subjects.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

NONE

Enrollment

Conditions

Opioid Overdose

Interventions

Nalmefene + 0.94% MgCl2DRUG

Nalmefene 0.5 mg + 0.94% MgCl2 for IV (bolus) administration

Nalmefene + 0.94% MgCl2DRUG

Nalmefene 0.5 mg + 0.94% MgCl2 for IM administration

Nalmefene Hydrochloride InjectionDRUG

Nalmefene Hydrochloride Injection 0.5 mg for IV (bolus) administration

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

Key Inclusion criteria: 1. Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring. 2. Body weight ranging from 50 to 100 kg (110-220 lbs) inclusive at screening and body mass index (BMI) within the range \[18.0-30.0\] kg/m2 (inclusive). 3. Willing to be compliant with the protocol, are able to read, understand, and answer verbal questions. Key Exclusion criteria: 1. Females who are pregnant or lactating. 2. Current or recent (within 5 years) history of drug or alcohol abuse. 3. History or any current conditions that might interfere with drug absorption, distribution, metabolism or excretion. 4. Known allergy or hypersensitivity to nalmefene hydrochloride or any of the excipients or other drug product components of nalmefene hydrochloride. 5. Dosing in a clinical drug study during the 30 days preceding the initial dose in this study. 6. Any significant illness during the 30 days preceding the initial dose in this study Other inclusion/exclusion criteria may apply.

Locations (1)

Ohio Clinical Trials

Columbus, Ohio, United States

Outcomes

Primary Outcomes

Area Under the Curve (AUC0-2.5)

Partial area under the plasma concentration-time curve from time zero to 2.5 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 2.5 minutes post-dose

Area Under the Curve (AUC0-5)

Partial area under the plasma concentration-time curve from time zero to 5 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 5 minutes post-dose

Area Under the Curve (AUC0-10)

Partial area under the plasma concentration-time curve from time zero to 10 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 10 minutes post-dose

Area Under the Curve (AUC0-15)

Partial area under the plasma concentration-time curve from time zero to 15 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 15 minutes post-dose

Area Under the Curve (AUC0-20)

Partial area under the plasma concentration-time curve from time zero to 20 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 20 minutes post-dose

Area Under the Curve (AUC0-30)

Partial area under the plasma concentration-time curve from time zero to 30 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: 30 minutes post-dose

Data from ClinicalTrials.gov

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Area Under the Curve (AUCt)

Area under the plasma concentration-time curve from time zero to the time of last measurable concentration following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: Up to 48 hours post-dose

Area Under the Curve (AUCinf)

Area under the plasma concentration-time curve from time zero to infinity following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: Up to 48 hours post-dose

Maximum Plasma Concentration (Cmax)

Maximum plasma concentration of nalmefene following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene hydrochloride injection 0.5 mg IV bolus administration

Time frame: Up to 48 hours post-dose

Area Under the Curve (AUC0-2.5)

Partial area under the plasma concentration-time curve from time zero to 2.5 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 2.5 minutes post-dose

Area Under the Curve (AUC0-5)

Partial area under the plasma concentration-time curve from time zero to 5 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 5 minutes post-dose

Area Under the Curve (AUC0-10)

Partial area under the plasma concentration-time curve from time zero to 10 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 10 minutes post-dose

Area Under the Curve (AUC0-15)

Partial area under the plasma concentration-time curve from time zero to 15 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 15 minutes post-dose

Area Under the Curve (AUC0-20)

Partial area under the plasma concentration-time curve from time zero to 20 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 20 minutes post-dose

Area Under the Curve (AUC0-30)

Partial area under the plasma concentration-time curve from time zero to 30 minutes following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: 30 minutes post-dose

Area Under the Curve (AUCt)

Time frame: Up to 48 hours post-dose

Area Under the Curve (AUCinf)

Area under the plasma concentration-time curve from time zero to infinity following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: Up to 48 hours post-dose

Maximum Plasma Concentration (Cmax)

Maximum plasma concentration of nalmefene following nalmefene 0.5 mg (0.94% MgCl2) IV bolus administration and nalmefene 0.5 mg (0.94% MgCl2) IM administration

Time frame: Up to 48 hours post-dose