Study to Evaluate Multiple Doses of Fluconazole, a CYP3A4 and CYP2C9 Inhibitor, on the Pharmacokinetics of CTP-543 in Healthy Subjects

A Phase 1, Open-Label, Fixed-Sequence, Drug-Drug Interaction Study to Evaluate the Effect of Multiple Doses of Fluconazole, a CYP3A4 and CYP2C9 Inhibitor, on the Pharmacokinetics of CTP-543 in Healthy Subjects

A single center, Phase 1, open-label, fixed-sequence, drug-drug interaction study to evaluate the effect of multiple doses of Fluconazole, a CYP3A4 and CYP2C9 inhibitor, on the pharmacokinetics (PK) of CTP-543 in healthy subjects

Study Overview

• Status: Completed
• Conditions: Health Volunteers
• Intervention / Treatment: Drug: CTP-543; Drug: Fluconazole

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Florida
    • Miami, Florida, United States, 33014
      • Clinical Pharmacology of Miami, LLC

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy, adult, male or female, aged 18-60 inclusive
• Non-smoker who has not used nicotine-containing products for at least 3 months prior to the first dosing
• Body mass index (BMI) ≥ 18.0 and ≤ 32.0 kg/m2 at screening
• If of reproductive age, willing and able to use a medically highly effective form of birth control 4 weeks prior to first dose, during the study and for 30 days following last dose of study medication.
• Understands the study procedures in the informed consent form (ICF), and be willing and able to comply with the protocol

Exclusion Criteria:

• History or presence of clinically significant medical or psychiatric condition or disease
• History or presence of alcohol or drug abuse within the past 2 years
• History or presence of hypersensitivity or idiosyncratic reaction to the study drugs or related compounds
• Presence or history of significant gastrointestinal, liver or kidney disease, or any other condition that is known to interfere with drug absorption, distribution, metabolism or excretion, or known to potentiate or predispose to undesired effects
• History of prolonged QT syndrome or a QTc interval with Fridericia's correction (QTcF) > 450 msec for males or QTcF > 470 msec for females at Screening visit or prior to the first dosing
• Abnormal liver function at Screening
• Females who are nursing, pregnant, or planning to become pregnant while in the study, and for 30 days after last dose of study drug
• Positive results for coronavirus infection (COVID-19) at Screening or check-in
• Positive drug or alcohol results at Screening or check-in
• Positive results at Screening for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg) or hepatitis C virus (HCV)
• Vaccination with a live attenuated vaccine up to 6 weeks prior to dosing. Live vaccines include (but are not limited to) the measles, mumps, and rubella (MMR) vaccine; intranasal flu vaccine; and Zostavax for herpes zoster

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: CTP-543 and Fluconazole Treatment; On Day 1, each subject will receive a single oral dose of 12 mg CTP-543. Following a washout on Day 2, each subject will receive an oral dose of 200 mg fluconazole once daily on Days 3 through to Day 8. On Day 7, approximately 1 hour after the 200 mg dose of fluconazole, each subject will receive a single oral dose of 12 mg CTP-543.	Drug: CTP-543; 12 mg on Day 1 and Day 7; Drug: Fluconazole; 200 mg once daily on Days 3 through to Day 8

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	Maximum observed concentration	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose
Tmax	Time to reach maximum observed concentration	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose
λz	Terminal elimination rate constant	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose
t1/2	Apparent terminal half-life	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose
AUC0-tlast	Area under the concentration-time curve from time 0 to the time of the last observed/measured non-zero concentration	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose
AUC0-inf	Area under the concentration-time curve from time 0 extrapolated to infinity	Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Assessment of Safety and Tolerability following administration of CTP-543	Number of adverse events, including abnormal clinical laboratory findings, abnormal physical examinations, abnormal ECGs and abnormal vital signs tabulated for each subject	Continuous from screening (within 21 days prior to Day 1) through Discharge (approximately 7 days after last study drug administration)

Collaborators and Investigators

• Sponsor: Concert Pharmaceuticals

Study record dates

Study Major Dates

• Study Start (Actual): July 11, 2022
• Primary Completion (Actual): August 6, 2022
• Study Completion (Actual): August 12, 2022

Study Registration Dates

• First Submitted: July 26, 2022
• First Submitted That Met QC Criteria: July 26, 2022
• First Posted (Actual): July 28, 2022

Study Record Updates

• Last Update Posted (Actual): August 30, 2022
• Last Update Submitted That Met QC Criteria: August 29, 2022
• Last Verified: August 1, 2022

More Information

Terms related to this study

• Keywords: CTP-543
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Enzyme Inhibitors; Hormones, Hormone Substitutes, and Hormone Antagonists; Cytochrome P-450 Enzyme Inhibitors; Hormone Antagonists; Antifungal Agents; Steroid Synthesis Inhibitors; 14-alpha Demethylase Inhibitors; Cytochrome P-450 CYP2C9 Inhibitors; Cytochrome P-450 CYP2C19 Inhibitors; Fluconazole
• Other Study ID Numbers: CP543.1015

Drug and device information, study documents

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