CG-549 Tablet Pharmacokinetics Study

CG-549 Tablet Pharmacokinetics Study: An Open-label, Single Ascending Dose Study to Evaluate the Safety and Pharmacokinetics of a Tablet Formulation of CG-549 in Healthy Subjects

This will be an open label, crossover, single dose study consisting of 2 parts (Part A and Part B) in a total of 24 healthy male and female subjects.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: CG-549

Detailed Description

Part A Part A is an open-label, 3-period, fixed-sequence, escalating dose study in 6 healthy subjects to find a tablet dose that results in a CG-549 exposure that is expected to be safe and potentially efficacious (i.e., within the targeted efficacious exposure range as defined below).

Subjects will receive the following treatments of the tablet formulation of CG-549, in the fed state:

• Period 1: a single oral dose of 300 mg CG-549 on Day 1.
• Period 2: a single oral dose of XX mg CG-549 on Day 1. After interim PK evaluation of Period 1, the CG-549 dose of Period 2 will aim at reaching the lower end of the targeted efficacious exposure range.
• Period 3: a single oral dose of YY mg CG-549 on Day 1. After interim PK evaluation of Period 2, the CG-549 tablet dose of Period 3 will aim at reaching the higher end of the targeted efficacious exposure range.

Doses XX and YY will be multiples of 300 mg and will not exceed 3 times the dose used in the preceding period.

After interim PK evaluation of all periods in Part A, the CG-549 dose and the type of breakfast to be used in Part B will be selected which is anticipated to result in an exposure that is expected to be safe and potentially efficacious.

Part B Part B is an open-label, 2-period, randomized crossover study in 18 healthy subjects to confirm that the selected dose of the tablet formulation of CG-549 results in a CG-549 exposure that is expected to be safe and potentially efficacious, and to compare the PK profiles of a single dose of the tablet formulation of CG 549 between the fed and the fasted states.

Subjects will receive the following treatments of the tablet formulation of CG-549:

• Period 1: a single oral dose of ZZ mg CG-549 on Day 1 in fed or fasted state.
• Period 2: a single oral dose of ZZ mg CG-549 on Day 1 in fasted or fed state. Dose ZZ will be a multiple of 300 mg.

There will be 2 treatment sequences in the study: fed-fasted and fasted-fed. Subjects will be randomly assigned to a treatment sequence in a 1:1 ratio. In the fed state, subjects will either receive a high-fat or a medium fat breakfast.

• Study Type: Interventional
• Enrollment (Actual): 24
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands
    • PRA Health Sciences (PRA) - Early Development Services (EDS)

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:

1. Sex:Males and females
2. Age:18 to 55 years, inclusive, at screening
3. Weight:≥50 kg, at screening
4. Body mass index:18.0 to 30.0 kg/m2, inclusive, at screening
5. Smoking behavior :Non-smoking or smoking ≤5 cigarettes, 1 cigar, or 1 pipe per day
6. Other criteria:Liver enzymes within the normal range and creatine phosphokinase within 2.0 times the normal range

Key Exclusion Criteria:

1. Previous participation in the current study.
2. Employee of PRA or the Sponsor.
3. History of bacterial or viral infection requiring treatment with antibiotics or antivirals within 1 month prior to screening.
4. Presence or history of esophageal or gastroduodenal ulceration within 1 month prior to screening.
5. Significant and/or acute illness within 5 days prior to the first drug administration that may impact safety assessments, in the opinion of the Investigator.

Study Plan

How is the study designed?

Design Details

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

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: fed state in PART B	Drug: CG-549; PART A (open-label) Period 1: single oral dose. Period 2: After PK evaluation of period 1. Period 3: After PK evaluation of period 2. PART B (randomized); Period 1: a single oral dose of ZZ mg CG-549 on Day 1 in fed or fasted state.; Period 2: a single oral dose of ZZ mg CG-549 on Day 1 in fasted or fed state.; Other Names: PART A and PART B
Experimental: fasted state in PART B	Drug: CG-549; PART A (open-label) Period 1: single oral dose. Period 2: After PK evaluation of period 1. Period 3: After PK evaluation of period 2. PART B (randomized); Period 1: a single oral dose of ZZ mg CG-549 on Day 1 in fed or fasted state.; Period 2: a single oral dose of ZZ mg CG-549 on Day 1 in fasted or fed state.; Other Names: PART A and PART B

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum Observed Plasma Concentration (Cmax) of CG549	up to 4 weeks
Area Under the Concentration-Time Curve (AUC) of CG549	up to 4 weeks

Secondary Outcome Measures

Outcome Measure	Time Frame
The Number of Participants Who Experienced Serious or Non-Serious Adverse Events	up to 4 weeks

Collaborators and Investigators

• Sponsor: CrystalGenomics, Inc.
• Investigators: Principal Investigator: Maria Velinova, Ph.D, PRA Health Sciences (PRA) - Early Development Services (EDS)

Study record dates

Study Major Dates

• Study Start (Actual): September 23, 2019
• Primary Completion (Actual): January 20, 2020
• Study Completion (Actual): June 30, 2020

Study Registration Dates

• First Submitted: December 10, 2019
• First Submitted That Met QC Criteria: May 24, 2022
• First Posted (Actual): May 26, 2022

Study Record Updates

• Last Update Posted (Actual): May 26, 2022
• Last Update Submitted That Met QC Criteria: May 24, 2022
• Last Verified: May 1, 2022

More Information

Terms related to this study

• Other Study ID Numbers: CG-549-1-03

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No