Single-dose to Evaluate the Pharmacokinetics of GTX-101 and Subcutaneous Injectable Bupivacaine in Healthy Subjects

Parallel Study to Evaluate the Pharmacokinetics, Dose Proportionality, Safety and Tolerability of GTX-101 (Bupivacaine Hydrochloride Metered Dose Spray) and Subcutaneous Injectable Bupivacaine in Healthy Subjects

This is a single-center, randomized, single-dose, active-controlled study in healthy male and female subjects.

The study will enroll subjects to evaluate the PK of 3 dose strengths (50 mg, 100 mg and 200 mg) of GTX-101 compared to Subcutaneous injection in healthy adult subjects.

Blood samples for PK assessments will be collect at specified time points. Safety assessments will also be performed throughout the study.

Study Overview

• Status: Active, not recruiting
• Conditions: Postherpetic Neuralgia
• Intervention / Treatment: Drug: GTX-101; Drug: Bupivacaine HCl subcutaneous injection

• Study Type: Interventional
• Enrollment (Actual): 48
• Phase: Phase 1

Contacts and Locations

Study Locations

• Canada
  • Montréal, Canada
    • Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Provision of signed and dated informed consent form (ICF)
• Healthy adult male or female, aged 18 to 55 years, inclusive, at Screening
• Body mass index (BMI) within 18.0 kg/m2 to 30.0 kg/m2, inclusively at Screening
• Have no clinically significant diseases captured in the medical/surgical history or evidence of clinically significant findings on the physical examination (including vital signs), weight and/or clinical laboratory tests and/or ECG, as determined by an Investigator

Exclusion Criteria:

• History of significant hypersensitivity to bupivacaine, local anesthetic agents of amide type, or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (like angioedema) to any drugs
• Presence of significant gastrointestinal, liver or kidney disease, or any other conditions known to interfere with the absorption, distribution, metabolism or excretion of drugs or known to potentiate or predispose to undesired effects
• History of significant gastrointestinal, liver or kidney disease that may affect drug bioavailability

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

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 50 mg GTX-101	Drug: GTX-101; Bupivacaine HCl metered spray; Other Names: Bupivacaine HCl metered spray
Experimental: 100 mg GTX-101	Drug: GTX-101; Bupivacaine HCl metered spray; Other Names: Bupivacaine HCl metered spray
Experimental: 200 mg GTX-101	Drug: GTX-101; Bupivacaine HCl metered spray; Other Names: Bupivacaine HCl metered spray
Active Comparator: Bupivacaine subcutaneous injection	Drug: Bupivacaine HCl subcutaneous injection; Bupivacaine HCl, 50 mg/10 mL

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax between 0 hour to 240 hour after study drug administration	Maximum concentration occuring at Tmax	From 0 hour to 240 hour after study drug administration
Tmax between 0 hour to 240 hour after study drug administration	Time of maximum observed concentration	From 0 hour to 240 hour after study drug administration
AUC last	Area under the concentration time curve from the time of last dosing to the time of last quantifiable concentration (Tlast)	From 0 hour to 240 hour after study drug administration
AUC inf	Area under the concentration time curve extrapolated to infinity	From 0 hour to 240 hour after study drug administration

Collaborators and Investigators

• Sponsor: Acasti Pharma Inc.

Study record dates

Study Major Dates

• Study Start (Actual): July 26, 2022
• Primary Completion (Actual): August 21, 2022
• Study Completion (Anticipated): May 3, 2023

Study Registration Dates

• First Submitted: July 14, 2022
• First Submitted That Met QC Criteria: August 24, 2022
• First Posted (Actual): August 26, 2022

Study Record Updates

• Last Update Posted (Actual): January 23, 2023
• Last Update Submitted That Met QC Criteria: January 20, 2023
• Last Verified: June 1, 2022

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Nervous System Diseases; Pain; Neurologic Manifestations; Neuromuscular Diseases; Peripheral Nervous System Diseases; Neuralgia; Neuralgia, Postherpetic; Physiological Effects of Drugs; Central Nervous System Depressants; Peripheral Nervous System Agents; Sensory System Agents; Anesthetics; Anesthetics, Local; Bupivacaine
• Other Study ID Numbers: GTX-101-004

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