Evaluation of the PK Profile of Firibastat Following Administration of Firibastat Prototype Tablet Formulations

A Study in Healthy Subjects Designed to Evaluate the Pharmacokinetic Profile of Firibastat (QGC001) and Active Metabolites Following Administration of Firibastat (QGC001) Prototype Tablet Formulations

This is a single-centre, open-label, non-randomised, period fixed sequence study designed to investigate the PK and safety of Firibastat (QGC001) modified release (MR) prototype tablet formulations and compare this to a reference Firibastat (QGC001) immediate release (IR) capsule formulation in healthy male subjects.

It is planned to enrol 12 subjects to receive single oral doses of investigational medicinal product (IMP).

Study Overview

• Status: Completed
• Conditions: Healthy Males
• Intervention / Treatment: Drug: Firibastat

Detailed Description

Subjects will be screened for eligibility to participate in the study up to 28 days before dosing and for each treatment period they will be admitted to the clinical unit on the evening prior to IMP administration (Day -1). On the morning of Day 1, subjects will receive IMP in the fasted state (or following a FDA standard high-fat breakfast, if applicable) and will remain on site until 48 h post-dose. Between the periods, an interim analysis and review of safety and PK data from dosed regimens will be performed in order to determine which Firibastat (QGC001) MR prototype tablet formulation and dose to administer in subsequent periods. A follow-up phone call will take place 7 to 10 days post-final dose to ensure the ongoing wellbeing of the subjects.

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Nottingham, United Kingdom
    • Quotient Sciences

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

• Body mass index of 18.0 to 32.0 kg/m2
• Must adhere to the contraception requirements

Exclusion Criteria:

• Subjects who have received any IMP in a clinical research study within the previous 3 months
• Subjects with pregnant partners
• History of any drug or alcohol abuse in the past 2 years
• Clinically significant abnormal biochemistry, haematology or urinalysis
• Subjects with BP <90/50 mmHg at screening

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Interventional Model: Sequential Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Firibastat prototype tablet formulations; Firibastat (QGC001) 500 mg modified release prototype tablet formulations or immediate release capsule formulation - 1 tablet or 1 capsule administered per period	Drug: Firibastat; Firibastat (QGC001) 500 mg; Other Names: QGC001

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the Maximum Plasma Concentration.	[Cmax]	3 months
Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the time at which the Cmax is observed.	[Tmax]	3 months
Pharmacokinetic (PK) profiles of Firibastat (QGC001) and active métabolites of modified release prototype tablet formulations. Assessment of the Areas Under the Curve.	[AUC0-24, AUC0-last and AUC0-inf]	3 months

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Relative bioavailability of Firibastat (QGC001) modified release prototype tablet formulations compared to the immediate release capsule formulation	[AUC0-24 MR / AUC0-24 IR]	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing safety haematology and chemistry laboratory tests aggregated as number of patients outside normal ranges.	Basophils, Eosinophils, Haematocrit, Haemoglobin, Lymphocytes, Mean Cell, Haemoglobin, Mean Cell Haemoglobin Concentration, Mean Cell Volume, Monocytes, Neutrophils, Platelet Count, Red Blood Cell Count, White Blood Cell Count	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing chemistry laboratory tests aggregated as number of patients outside normal ranges.	Alanine Aminotransferase, Albumin, Alkaline Phosphatase, Aspartate Aminotransferase, Bicarbonate, Bilirubin (Total), Calcium, Chloride, Creatine Kinase, Gamma Glutamyl Transferase, Glucose (Fasting), Potassium, Phosphate (Inorganic), Protein (Total), Sodium, Urea	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing urinalysis aggregated as number of patients outside normal ranges.	Bilirubin, Blood, Glucose, Ketones, Leukocytes, Nitrites, pH, Protein, Specific gravity, Urobilinogen	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing vital signs	Blood pressure (mmHg)	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing vital signs	Heart rate (bpm)	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing AEs	Adverse events will be recorded from the time of providing written informed consent until discharge from the study at the follow-up visit. During each study visit the subject will be questioned directly regarding the occurrence of any adverse medical event according to the source schedule.	3 months
Safety and tolerability of single doses of Firibastat (QGC001) by assessing Twelve-lead ECGs	P wave, T wave, QRS complex, QT interval, RR interval, PR segment, ST segment,	3 months

Collaborators and Investigators

• Sponsor: Quantum Genomics SA
• Collaborators: Quotient Sciences

Study record dates

Study Major Dates

• Study Start (Actual): February 15, 2019
• Primary Completion (Actual): May 15, 2019
• Study Completion (Actual): June 7, 2019

Study Registration Dates

• First Submitted: September 26, 2018
• First Submitted That Met QC Criteria: October 18, 2018
• First Posted (Actual): October 22, 2018

Study Record Updates

• Last Update Posted (Actual): June 18, 2019
• Last Update Submitted That Met QC Criteria: June 17, 2019
• Last Verified: June 1, 2019

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Antihypertensive Agents; Firibastat
• Other Study ID Numbers: QGC001-1QG3; QSC118052 (Other Identifier: Quotient Sciences); 2018-001909-89 (EudraCT Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: Undecided

Drug and device information, study documents

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