Bioavailability of Levoketoconazole and Ketoconazole Tablets

NCT04212000 | Completed Phase 1 FDA Drug

• 1 other identifier: LKC101A
• Study Type: interventional
• Target: 34
• Locations: 1 country
• Sites: 1

Brief Summary

This is a phase 1, randomized, open-label, single-dose, two-period, two-sequence crossover study in healthy male and female subjects to evaluate the relative oral bioavailability of levoketoconazole tablets (the test drug) and ketoconazole tablets (the reference drug product).

Conditions

Healthy

Outcome Measures

Primary Outcomes (3)

• Ratio of geometric least squares means for AUClast of plasma levoketoconazole (2S,4R-ketoconazole)

  Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)

  24 hours

• Ratio of geometric least squares means for AUCinf of plasma levoketoconazole (2S,4R-ketoconazole)

  Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)

  24 hours

• Ratio of geometric least squares means for Cmax of plasma levoketoconazole (2S,4R-ketoconazole)

  Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)

  24 hours

Secondary Outcomes (8)

• Terminal phase rate constant (λz)

  24 hours

• Time to Maximum Plasma concentration (Tmax)

  24 hours

• Lag-time (Tlag)

  24 hours

• Apparent systemic clearance (CL/F)

  24 hours

• The percentage of area under the plasma concentration-time curve extrapolated from time 0 to infinity as a percentage of total AUC (%AUCext)

  24 hours

Study Arms (2)

Levoketoconazole

EXPERIMENTAL

Levoketoconazole 150 mg

Drug: Levoketoconazole

Ketoconazole

ACTIVE COMPARATOR

Ketoconazole 200 mg

Drug: Ketoconazole

Interventions

Levoketoconazole DRUG

Levoketoconazole tablet

Also known as: COR-003

Levoketoconazole

Ketoconazole DRUG

Ketoconazole tablet

Ketoconazole

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• to 55 years of age, inclusive, at time of consent.
• Body mass index (BMI) between 18.0 and 32.0 kg/m2,inclusive.
• In good general physical health as determined by absence of clinically significant medical history, physical examination findings, vital signs, clinical laboratory evaluations, and ECG measurements.
• Has not consumed and agrees to abstain from taking any prescription drugs, dietary supplements including vitamins and herbal preparations, or non-prescription drugs for 14 days prior to clinical research unit (CRU) admission, during washout period, and through Follow-Up.
• Has not consumed alcohol-containing beverages for 3 days prior to CRU admission and agrees not to consume alcohol through Follow-Up.
• Is a nonsmoker (for at least 3 months) with negative urinary cotinine test at Screening and agrees to abstain from tobacco-and nicotine-containing products for the duration of the study.

You may not qualify if:

• Evidence of any out-of-normal-range laboratory value at Screening that has not been reviewed, approved, and documented as Not Clinically Significant by the Investigator.
• Concurrent medical illness that would interfere with the conduct of the study in the opinion of the Investigator.
• History or presence of clinically significant cardiovascular, pulmonary, hematologic, endocrine, immunologic, dermatologic, neurologic, psychiatric, renal, hepatic, chronic respiratory, or gastrointestinal disease as judged by the Investigator.
• Positive urine drug screen for drugs-of-abuse, including cocaine, tetrahydrocannabinol, opioids, benzodiazepines, amphetamines, and barbiturates,and/or positive urine screen for alcohol at Screening and CRU admission.
• Treatment with an investigational drug within the longer of 30 days or five half-lives of the investigational drug preceding the first dose of study drug.
• Positive for HIV, hepatitis B, and/or hepatitis C on Screening assessments.
• Acute illness within 7 days of CRU admission.
• Donated plasma within 7 days of drug administration.
• Donated 1 or more pints of blood (or equivalent blood loss) within 30 days prior to drug administration.
• History of caffeine consumption exceeding 8 cups coffee/day within 14 days prior to first dose, or consumption of any caffeine-or chocolate-containing products for 3 days prior to CRU admission each week.
• Female subjects who are pregnant or lactating.
• Males with hemoglobin less than 12.0 g/dL at Screening or CRU admission; Females with hemoglobin less than 11.0 g/dL at Screening or CRU admission
• Had difficulties with swallowing whole tablets.
• Body habitus preventing repeated venipuncture as required by protocol.

Sponsors & Collaborators

• Cortendo AB: lead

Study Sites (1)

Pharmaceutical Research Associates, Inc.

Salt Lake City, Utah, 84124, United States

Location

MeSH Terms

Interventions

Ketoconazole

Intervention Hierarchy (Ancestors)

Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Xavier Valencia, MD

  Cortendo AB

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 11, 2019
• First Posted: December 26, 2019
• Study Start: December 16, 2019
• Primary Completion: January 18, 2020
• Study Completion: January 23, 2020
• Last Updated: January 31, 2020

Record last verified: 2020-01

Locations

US (1)