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

Phase 1

Completed

• Conditions: Healthy Subjects
• Interventions: Drug: Norketotifen Oral Capsule (Cohort 3); Drug: Norketotifen Oral Capsule (Multiple Dose Cohort); Drug: Norketotifen Oral Capsule (Cohort 1); Drug: Norketotifen Oral Capsule (Cohort 2); Drug: Placebo Oral Capsule

• Registration Number: NCT03712163
• Lead Sponsor: Emergo Therapeutics, Inc.

Brief Summary

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.

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 Timeline

• Study First Submitted: 2018-10-12
• Study Start: 2018-10-15
• Study First Submitted QC: 2018-10-17
• Study First Posted: 2018-10-19
• Primary Completion: 2019-02-18
• Status Verified: 2019-03
• Study Completion: 2019-03-14
• Last Update Submitted: 2019-03-19
• Last Update Posted: 2019-03-21

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 74

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 & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Norketotifen or Placebo (Cohort 2)	Placebo Oral Capsule	-
Norketotifen or Placebo (Cohort 3)	Norketotifen Oral Capsule (Cohort 3)	-
Norketotifen or Placebo (Cohort 3)	Placebo Oral Capsule	-
Norketotifen or Placebo (Multiple Dose)	Norketotifen Oral Capsule (Multiple Dose Cohort)	-
Norketotifen or Placebo (Multiple Dose)	Placebo Oral Capsule	-
Norketotifen or Placebo (Cohort 1)	Norketotifen Oral Capsule (Cohort 1)	-
Norketotifen or Placebo (Cohort 1)	Placebo Oral Capsule	-
Norketotifen or Placebo (Cohort 2)	Norketotifen Oral Capsule (Cohort 2)	-

Primary Outcome Measures

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

Secondary Outcome Measures

Name	Time	Method
Maximum plasma concentration (Cmax) following single doses	Through Day 4
Area under the plasma concentration time curve (AUC) following multiple doses	Through Day 7
Apparent clearance (CL/F) 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
Apparent clearance (CL/F) following single doses	Through Day 4
Maximum plasma concentration (Cmax) 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 volume of distribution (Vz/F) following multiple doses	Through Day 7
Area under the plasma concentration time curve (AUC) following single doses	Through Day 4
Apparent volume of distribution (Vz/F) following single doses	Through Day 4

Trial Locations

Locations (1)

Worldwide Clinical Trials; 🇺🇸 San Antonio, Texas, United States