Study to Investigate Effect of Food and Safety of a New Formulation of Zoliflodacin

NCT03718806 | Completed Phase 1 FDA Drug

• 1 other identifier: STI_ZOLI002
• Study Type: interventional
• Target: 48
• Locations: 1 country
• Sites: 1

Brief Summary

This is a phase I, parallel, open-label, randomized, cross-over, single-center study with zoliflodacin administered as granules for oral suspension with or without food. It is planned to enroll 2 cohorts (Cohorts 1 and 2) of 24 subjects each (48 subjects in total), with the target of achieving data in 20 evaluable subjects per cohort. Single doses of zoliflodacin will be assessed within each cohort in a two period cross-over design. Each subject will receive one of the following regimens per period, depending on cohort, in a sequence according to the randomization schedule (per cohort, subjects will be randomized immediately before dosing in Period 1), separated by a minimum 4 day washout between each period. The actual length of washout period may change pending emerging PK data. Cohort 1:

• Regimen A: 3 g zoliflodacin oral suspension; oral administration after an overnight fast
• Regimen B: 3 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast Cohort 2
• Regimen C: 4 g zoliflodacin oral suspension; oral administration after an overnight fast
• Regimen D: 4 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast

Conditions

Gonorrhea

Outcome Measures

Primary Outcomes (4)

• PK parameter of zoliflodacin : Cmax

  the maximum observed concentration of zoliflodacin after a single oral 3 g dose and a single oral 4 g dose administered as granules for oral suspension in healthy male and female subjects

  Day 3

• PK parameter of zoliflodacin : Tmax

  Tmax (the elapsed time from dosing at which Cmax was apparent) of zoliflodacin after a single oral 3 g dose and a single oral 4 g dose administered as granules for oral suspension in healthy male and female subjects

  Day 3

• PK parameter of zoliflodacin : AUC

  Area Under the Curve of zoliflodacin after a single oral 3 g dose and a single oral 4 g dose administered as granules for oral suspension in healthy male and female subjects

  Day 3

• PK parameter of zoliflodacin : T1/2

  the apparent elimination half-life of zoliflodacin after a single oral 3 g dose and a single oral 4 g dose administered as granules for oral suspension in healthy male and female subjects

  Day 3

Secondary Outcomes (4)

• safety and tolerability of zoliflodacin

  end of study

• relative bioavailability (Cmax) of zoliflodacin in the fed and fasted states

  Day 3

• relative bioavailability (AUC) of zoliflodacin in the fed and fasted states

  Day 3

• zoliflodacin effect on QT intervals

  Day 2

Study Arms (4)

Regimen A

EXPERIMENTAL

3 g zoliflodacin oral suspension; oral administration after an overnight fast

Drug: Zoliflodacin

Regimen B

EXPERIMENTAL

3 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast

Drug: Zoliflodacin; Other: high calorie, high fat breakfast

Regimen C

EXPERIMENTAL

4 g zoliflodacin oral suspension; oral administration after an overnight fast

Drug: Zoliflodacin

Regimen D

EXPERIMENTAL

4 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast

Drug: Zoliflodacin; Other: high calorie, high fat breakfast

Interventions

Zoliflodacin DRUG

oral suspension; oral administration

Regimen A; Regimen B; Regimen C; Regimen D

high calorie, high fat breakfast OTHER

fasted/fed conditions

Regimen B; Regimen D

Eligibility Criteria

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

You may qualify if:

• Healthy males or non-pregnant, non-lactating healthy females
• Age 18 to 55 years of age
• Body mass index of 18.0 to 30.1 kg/m2
• Light smokers (less than 5 cigarettes per day) or subjects who are nonsmokers. No smoking (or use of smoking substitute e.g. nicotine patch) is permitted from screening throughout the study
• Normal arterial BP and HR or, if abnormal, considered not clinically significant by the PI. These will be measured after resting supine for 10 min
• Registered in agreement with the applicable law on biomedical experimentation
• Must be willing and able to comply with all study requirements
• Must be able to understand a written informed consent, which must be obtained prior to initiation of study procedures
• Must agree to use an adequate method of contraception
• Must, in the opinion of the investigator, be in good health based upon medical history and physical examination (including vital signs)

You may not qualify if:

• Subjects who have received of zoliflodacin or any IMP in a clinical research study within 5 half-lives or within 30 days prior to first dose. However, in no event, shall the time between last receipt of IMP and first dose be less than 3 months
• Subjects who are study site employees, or immediate family members of a study site or sponsor employee
• Subjects who have previously been enrolled in this study
• History of any drug or alcohol abuse in the past 2 years
• Regular alcohol consumption in males \>21 units per week and females \>14 units per week (1 unit = ½ pint beer, or a 25 mL shot of 40% spirit, 1.5 to 2 Units = 125 mL glass of wine, depending on type)
• Subjects who have regular daily consumption of ≥5 cigarettes daily, or use more than 3 grams (1/8 ounce) of tobacco
• Excessive intake of caffeine (more than 8 cups daily of beverage containing caffeine)
• Subjects who have regular daily consumption of more than one liter of xanthine containing beverages
• Females of childbearing potential who are pregnant or lactating (female subjects must have a negative serum pregnancy test at screening and admission)
• Have poor venous access that limits phlebotomy
• Clinically significant abnormal biochemistry, hematology or urinalysis at screening (i.e. aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, creatinine and urea must be within normal ranges) as judged by the investigator at screening and admission (laboratory parameters are listed in Appendix 1)
• Presence of clinically significant abnormality following review of vital signs, full physical examination and ECG
• Positive drugs of abuse test result
• History or presence of any clinically significant acute or chronic disease, including known or suspected human immunodeficiency virus (HIV), HBV or HCV infection
• Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance of \<80 mL/min using the Cockcroft-Gault equation

Sponsors & Collaborators

• Drugs for Neglected Diseases: lead
• Quotient Sciences: collaborator

Study Sites (1)

Quotient Sciences

Miami, Florida, 33126, United States

Location

MeSH Terms

Conditions

Gonorrhea

Interventions

zoliflodacin

Condition Hierarchy (Ancestors)

Neisseriaceae Infections; Gram-Negative Bacterial Infections; Bacterial Infections; Bacterial Infections and Mycoses; Infections; Sexually Transmitted Diseases, Bacterial; Sexually Transmitted Diseases; Communicable Diseases; Genital Diseases; Urogenital Diseases

Study Officials

• Juan Perez-Morales, MD

  Quotient Sciences

  PRINCIPAL INVESTIGATOR

Study Design

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

Model Details: It is planned to enroll 2 cohorts of 24 subjects each. Single doses of zoliflodacin (3 g and 4 g) will be assessed within each cohort in a two period cross-over design. Cohort 1 * Regimen A: 3 g zoliflodacin oral suspension; oral administration after an overnight fast * Regimen B: 3 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast Cohort 2 * Regimen C: 4 g zoliflodacin oral suspension; oral administration after an overnight fast * Regimen D: 4 g zoliflodacin oral suspension; oral administration with a standardized high calorie, high-fat breakfast There will be a minimum washout of 4 days between each period.

Study Record Dates

• First Submitted: October 17, 2018
• First Posted: October 24, 2018
• Study Start: October 3, 2018
• Primary Completion: November 12, 2018
• Study Completion: November 12, 2018
• Last Updated: December 6, 2018

Record last verified: 2018-10

Locations

US (1)