Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Norketotifen in Healthy Subjects

A Double-Blind, Placebo-Controlled, 2-Part, Single Ascending Dose and Multiple Dose Cohort Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Norketotifen in Healthy Subjects

This is a Phase 1, single-center, double-blind, randomized, placebo-controlled, 2-part, single ascending dose and multiple dose cohort study of orally administered Norketotifen (NKT) in healthy subjects.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: Norketotifen Oral Capsule (Cohort 1); Drug: Placebo Oral Capsule; Drug: Norketotifen Oral Capsule (Cohort 2); Drug: Norketotifen Oral Capsule (Cohort 3); Drug: Norketotifen Oral Capsule (Multiple Dose Cohort)

Detailed Description

Single Ascending Dose: Three single ascending dose cohorts are planned. A total of 10 subjects will be enrolled in each cohort and will be randomly assigned to receive a single oral dose of NKT (n=8) or a matching placebo (n=2). A Safety Review Team (SRT) will review all available safety data in a blinded manner following the completion of each cohort to determine the next dose level to be evaluated in the next cohort.

Multiple Dose Cohort: A total of 10 subjects will be enrolled and will be randomly assigned to receive multiple oral doses of NKT (n=8) or a matching placebo (n=2) once daily for an adequate number of days to reach steady state (the number of days will be determined based on the half-life of NKT in Part A). The dose of NKT to be evaluated will be determined by the SRT.

• Study Type: Interventional
• Enrollment (Actual): 74
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio, Texas, United States, 78217
      • Worldwide Clinical Trials

Participation Criteria

Eligibility Criteria

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

Description

Key Inclusion Criteria:

• Body mass index (BMI) of 18 to 30 kg/m^2
• Negative serum pregnancy test (females); females of childbearing potential and males must agree to use acceptable contraception

Key Exclusion Criteria:

• Pregnant or lactating (females)
• Clinically significant past or current medical or surgical history
• Clinically significant illness or abnormality on physical examination, 12-lead ECG, laboratory values
• Participation in an investigational drug or device study within 30 days prior to Screening

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Sequential Assignment
• Masking: Quadruple

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Norketotifen or Placebo (Cohort 1)	Drug: Norketotifen Oral Capsule (Cohort 1); Single dose Norketotifen; Drug: Placebo Oral Capsule; Placebo
Experimental: Norketotifen or Placebo (Cohort 2)	Drug: Placebo Oral Capsule; Placebo; Drug: Norketotifen Oral Capsule (Cohort 2); Single dose Norketotifen
Experimental: Norketotifen or Placebo (Cohort 3)	Drug: Placebo Oral Capsule; Placebo; Drug: Norketotifen Oral Capsule (Cohort 3); Single dose Norketotifen
Experimental: Norketotifen or Placebo (Multiple Dose)	Drug: Placebo Oral Capsule; Placebo; Drug: Norketotifen Oral Capsule (Multiple Dose Cohort); Multiple dose Norketotifen

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of subjects with adverse events following single doses	Including clinically significant and Grade 3 abnormalities in laboratory values, vital signs, ECGs, and physical examination	Through Day 4
Number of subjects with adverse events following multiple doses	Including clinically significant and Grade 3 abnormalities in laboratory values, vital signs, ECGs, and physical examination	Through Day 7

Secondary Outcome Measures

Outcome Measure	Time Frame
Maximum plasma concentration (Cmax) following single doses	Through Day 4
Maximum plasma concentration (Cmax) following multiple doses	Through Day 7
Time to maximum concentration (Tmax) following single doses	Through Day 4
Time to maximum concentration (Tmax) following multiple doses	Through Day 7
Area under the plasma concentration time curve (AUC) following single doses	Through Day 4
Area under the plasma concentration time curve (AUC) following multiple doses	Through Day 7
Elimination half-life (t1/2) following single doses	Through Day 4
Elimination half-life (t1/2) following multiple doses	Through Day 7
Apparent clearance (CL/F) following single doses	Through Day 4
Apparent clearance (CL/F) following multiple doses	Through Day 7
Apparent volume of distribution (Vz/F) following single doses	Through Day 4
Apparent volume of distribution (Vz/F) following multiple doses	Through Day 7

Collaborators and Investigators

• Sponsor: Emergo Therapeutics, Inc.
• Investigators: Principal Investigator: Cynthia Zamora, MD, Worldwide Clinical Trials

Study record dates

Study Major Dates

• Study Start (Actual): October 15, 2018
• Primary Completion (Actual): February 18, 2019
• Study Completion (Actual): March 14, 2019

Study Registration Dates

• First Submitted: October 12, 2018
• First Submitted That Met QC Criteria: October 17, 2018
• First Posted (Actual): October 19, 2018

Study Record Updates

• Last Update Posted (Actual): March 21, 2019
• Last Update Submitted That Met QC Criteria: March 19, 2019
• Last Verified: March 1, 2019

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Dermatologic Agents; Anti-Allergic Agents; Histamine H1 Antagonists; Histamine Antagonists; Histamine Agents; Antipruritics; Ketotifen
• Other Study ID Numbers: NKT-101

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