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Safety and Pharmacokinetics of a Novel Niclosamide Solution in Combination With Camostat

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: Placebo
Registration Number
NCT04644705
Lead Sponsor
Charité Research Organisation GmbH
Brief Summary

Niclosamide is a well-established substance that is a promising candidate for a repurposing approach to treat COVID-19. Niclosamide is currently marketed as a chewing tablet for the treatment of intestinal worm infections. The marketed formulation is optimized for minimal drug substance absorption. A niclosamide solution has been developed that is expected to release the drug substance more readily and more reproducibly.

Camostat is approved for oral treatment of chronic pancreatitis and reflux oesophagitis in Japan. Camostat has been shown to effectively block viral replication in a SARS-CoV-2 animal model. Since the mechanisms of actions are different, it was hypothesized that a combination of both substances might have an additive or even synergistic effect in the treatment of COVID-19 patients.

This 3-part study is designed to investigate (1) safety and pharmacokinetics of single ascending doses of the new niclosamide solution after fasted and fed conditions, (2) the relative bioavailability of the niclosamide solution compared to the chewing tablet, and (3) safety and pharmacokinetics of the combination of niclosamide solution and camostat after multiple doses in healthy volunteers.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
28
Inclusion Criteria
  • Healthy male or female subjects in good health as determined by past medical history
  • physical examination, vital signs and safety lab at screening
  • between 18 to 45 years of age
Exclusion Criteria
  • Significant illness
  • pregnant or lactating women

Study & Design

Study Type
INTERVENTIONAL
Study Design
FACTORIAL
Arm && Interventions
GroupInterventionDescription
Part A: placebo to niclosamidePlaceboThe SAD cohorts are planned as follows: Cohort A1: placebo to niclosamide 200 mg (fasted conditions) Cohort A2: placebo to niclosamide 600 mg (fasted conditions) Cohort A3: placebo to niclosamide 1600 mg (fasted and fed conditions)
Part C: placebo to niclosamide and camostatPlaceboSubjects will receive the combination of niclosamide solution (planned 500 mg three times daily) + camostat (600 mg three times daily) or placebo over a treatment period of 7 days. The dose of the niclosamide solution depends on the safety and pharmacokinetic results of Part A and B but will not exceed 500 mg three times daily.
Part A: verum niclosamideNiclosamideThe SAD cohorts are planned as follows: Cohort A1: 200 mg (fasted conditions) Cohort A2: 600 mg (fasted conditions) Cohort A3: 1600 mg (fasted and fed conditions)
Part B: verum as solution (niclosamide)NiclosamideTwo different crossover designs are chosen. Both are randomized, open-label, two-sequence, two periods crossover designs comparing the new niclosamide solution with the marketed chewing tablets. Planned doses are 1600 mg once daily (oral solution), 2000 mg once daily (chewing tablets) and 500 mg three times daily of both dosage forms.
Part B: verum as chewing tablet (niclosamide)NiclosamideTwo different crossover designs are chosen. Both are randomized, open-label, two-sequence, two periods crossover designs comparing the new niclosamide solution with the marketed chewing tablets. Planned doses are 1600 mg once daily (oral solution), 2000 mg once daily (chewing tablets) and 500 mg three times daily of both dosage forms.
Part C: verum (niclosamide and camostat)NiclosamideSubjects will receive the combination of niclosamide solution (planned 500 mg three times daily) + camostat (600 mg three times daily) or placebo over a treatment period of 7 days. The dose of the niclosamide solution depends on the safety and pharmacokinetic results of Part A and B but will not exceed 500 mg three times daily.
Primary Outcome Measures
NameTimeMethod
Maximum plasma concentration of niclosamide (µg/ml)from predose until 24 hours after intervention

Measurement will start at Day 1

Area Under the Plasma Concentration Time Curve from predose until last detectable concentration of niclosamide(AUC0-last) of niclosamide [µg/ml*h]from predose until 24 hours after intervention

Measurement will start at Day 1

Treatment emergent number of Adverse Eventsup to 14 days

Assessment of severity of an AE will be based on CTCAE Version 5.0

Secondary Outcome Measures
NameTimeMethod
Area Under the Plasma Concentration Time Curve between two dosing intervals (AUC tau ss) of niclosamide [µg/ml*h] at steady state after multiple dosingfrom predose until Day 9
Maximum plasma concentration of niclosamide (µg/ml) at steady state after multiple dosingfrom predose until Day 9
Food effect on maximum plasma concentration of niclosamide (µg/ml)from predose until 24 hours after intervention

Measurement will start at Day 1 after a standard high fat breakfast

Food effect on Area Under the Plasma Concentration Time Curve from predose until last detectable concentration of niclosamide (AUC0-last) [µg/ml*h]from predose until 24 hours after intervention

Measurement will start at Day 1 after a standard high fat breakfast

Trial Locations

Locations (1)

Charité Research Organisation GmbH

🇩🇪

Berlin, Germany

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