Comparison of the Relative Oral Bioavailability of GKT137831 Formulated in Capsules or in Tablets

Comparison of the Relative Oral Bioavailability of GKT137831 Formulated in Capsules or in Tablets and Evaluation of the Potential Impact of Concomitant Food Intake on the Relative Bioavailability of GKT137831 in Healthy Male Subjects

The study will be a comparative oral bioavailability study between GKT137831 capsules and tablets, together with an assessment of the impact of concomitant food intake on the relative bioavailability of GKT137831 tablets.

This will be a randomized three-way open cross-over study.

Study Overview

• Status: Completed
• Conditions: Phase 1
• Intervention / Treatment: Drug: GKT137831

• Study Type: Interventional
• Enrollment (Actual): 15
• Phase: Phase 1

Contacts and Locations

Study Locations

• France
  • Gières, France, 38610
    • Eurofins Optimed

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

1. Healthy male subject, aged 18 to 60 years inclusive;
2. Non-smoker subject or smoker of not more than 5 cigarettes a day ;
3. No history of alcohol or drug abuse
4. Body Mass Index (BMI) between 18 and 27 5 kg/m2 inclusive;
5. Considered as healthy after a comprehensive clinical assessment (detailed medical history and complete physical examination);
6. Signing a written informed consent prior to selection;

Exclusion Criteria:

1. Blood donation (including in the frame of a clinical study) within 2 months before administration;
2. General anaesthesia within 3 months before administration;
3. Presence or history of drug hypersensitivity, or allergic disease diagnosed and treated by a physician;
4. Inability to abstain from intensive muscular effort;
5. No possibility of contact in case of emergency;
6. Any drug intake (except paracetamol) during the last month prior to the first administration;
7. History or presence of drug or alcohol abuse (alcohol consumption > 40 grams / day);
8. Excessive consumption of beverages with xanthine bases (> 4 cups or glasses / day);
9. Positive Hepatitis B surface (HBs) antigen or anti Hepatitis C Virus (HCV) antibody, or positive results for Human Immunodeficiency Virus (HIV) 1 or 2 tests;
10. Positive results of screening for drugs of abuse;
11. Subject who, in the judgment of the Investigator, is likely to be non-compliant or uncooperative during the study, or unable to cooperate because of a language problem, poor mental development;
12. Exclusion period of a previous study;
13. Administrative or legal supervision;

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: Treatment A; Single oral dose of 400 mg GKT137831 administered as 4 x 100 mg capsules in fasting conditions.	Drug: GKT137831; oral bioavailable small molecule that selectively inhibit NOX1 and NOX4; Other Names: NOX1/4 inhibitor
Other: Treatment B: Single oral dose of 400 mg GKT137831 administered as 1 x 400 mg tablets in fasting conditions.	Drug: GKT137831; oral bioavailable small molecule that selectively inhibit NOX1 and NOX4; Other Names: NOX1/4 inhibitor
Other: Treatment C; Single oral dose of 400 mg GKT137831 administered as 1 x 400 mg tablets in fed conditions.	Drug: GKT137831; oral bioavailable small molecule that selectively inhibit NOX1 and NOX4; Other Names: NOX1/4 inhibitor

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Oral bioavailability (Fz)	To compare the relative oral bioavailability GKT137831 formulated in capsules or in tablets in healthy male subjects.	72 hours
Food effect on Oral bioavailability (Fz)	To assess the impact of concomitant food intake on the relative bioavailability of GKT137831 after single oral dose administration of a 400 mg GKT137831 tablet in healthy male subjects.	72 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of participants with treatment-related adverse events as assessed by CTCAE v5.0	To compare the safety and tolerability of single oral dose administration of 400 mg GKT137831 formulated in capsules or in tablets, and to evaluate the potential impact of concomitant food intake on the safety and tolerability of single oral dose administration of 400 mg GKT137831 tablet in healthy adult male subjects.	7 days
Oral bioavailability of GKT138184	To compare the relative oral bioavailability GKT138184 after oral administration of GKT137831 formulated in capsules or in tablets in healthy male subjects.	72 hours
Food effect on oral bioavailability of GKT138184	To assess the impact of concomitant food intake on the relative bioavailability of GKT138184 after single oral dose administration of a 400 mg GKT137831 tablet in healthy male subjects.	72 hours

Collaborators and Investigators

• Sponsor: Calliditas Therapeutics AB
• Collaborators: Eurofins Optimed; York Bioanalytical Solution

Study record dates

Study Major Dates

• Study Start (Actual): December 19, 2018
• Primary Completion (Actual): February 6, 2019
• Study Completion (Actual): February 6, 2019

Study Registration Dates

• First Submitted: October 12, 2018
• First Submitted That Met QC Criteria: November 9, 2018
• First Posted (Actual): November 14, 2018

Study Record Updates

• Last Update Posted (Actual): June 30, 2022
• Last Update Submitted That Met QC Criteria: June 27, 2022
• Last Verified: January 1, 2019

More Information

Terms related to this study

• Other Study ID Numbers: GSN000299

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