Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers

NCT02533102 | Completed Phase 1

• 1 other identifier: E7050-E044-004
• Study Type: interventional
• Target: 42
• Locations: 1 country
• Sites: 1

Brief Summary

This study is designed to first evaluate the effect of food on E7050's pharmacokinetic parameters following the administration of single 100 mg oral doses of E7050 tablet to each normal healthy participant in the study (Part A), and second to characterize E7050 pharmacokinetics after single doses at 200 mg and 400 mg under fasted conditions (Part B). Part A will be a randomized, single-dose, open-label, three-treatment period crossover study. Part B is a nonrandomized, open-label, two-treatment sequential study design. Twelve participants in Treatment Period 1 will receive a single dose of 200 mg of E7050 under fasted conditions. Following review of safety data of the 200 mg dose level, an additional 12 subjects will then receive a single dose of 400 mg of E7050 in Treatment Period 2.

Conditions

Healthy Subjects

Keywords

Pharmacokinetics; E7050; Healthy Subjects

Outcome Measures

Primary Outcomes (6)

• E7050 pharmacokinetic parameter: tmax (time to maximum plasma concentration)

  0 hour to 168 hours

• E7050 pharmacokinetic parameter: Cmax (maximum observed plasma concentration)

  0 hour to 168 hours

• E7050 pharmacokinetic parameter: t lag (time point immediately prior to the first quantifiable concentration)

  0 hour to 168 hours

• E7050 pharmacokinetic parameter: AUC 0-t (area under the plasma concentration-time profile from time 0 to the last measurable concentration)

  0 hour to 168 hours

• E7050 pharmacokinetic parameter: AUC 0-inf (area under the plasma concentration-time profile from time 0 to infinity)

  0 hour to 168 hours

• E7050 pharmacokinetic parameter: t1/2 (the terminal half-life)

  0 hour to 168 hours

Secondary Outcomes (1)

• Number of participants as a measure of adverse events (AEs) and serious adverse events (SAEs)

  Up to 9 weeks

Study Arms (5)

Part A: E7050 100 mg tablet under fasted conditions

EXPERIMENTAL

Participants will receive a single tablet containing 100 mg E7050 following an overnight fast.

Drug: E7050

Part A: E7050 100 mg tablet with low-fat breakfast

EXPERIMENTAL

Participants will receive a single tablet containing 100 mg E7050 with a standard low-fat meal.

Drug: E7050

Part A: E7050 100 mg tablet with high-fat breakfast

EXPERIMENTAL

Participants will receive a single tablet containing 100 mg E7050 with a standard high-fat meal.

Drug: E7050

Part B: E7050 200 mg tablet under fasted conditions

EXPERIMENTAL

Participants will receive a single dose of 200 mg (two 100 mg tablets) of E7050 under fasted conditions.

Drug: E7050

Part B: E7050 400 mg tablet under fasted conditions

EXPERIMENTAL

Participants will receive a single dose of 400 mg (four 100 mg tablets) of E7050 under fasted conditions.

Drug: E7050

Interventions

E7050 DRUG

100 mg tablet administered orally

Part A: E7050 100 mg tablet under fasted conditions; Part A: E7050 100 mg tablet with high-fat breakfast; Part A: E7050 100 mg tablet with low-fat breakfast; Part B: E7050 200 mg tablet under fasted conditions; Part B: E7050 400 mg tablet under fasted conditions

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Subjects must meet all of the following criteria to be included in this study:
• Normal healthy adult males and females (age 18-45 years).
• Body Mass Index (BMI) greater than or equal to 18 and less than or equal to 32 at the time of Screening.
• Non-smokers.
• Willing and able to comply with all aspects of the protocol.
• Provide written informed consent.

You may not qualify if:

• Participants who meet any of the following criteria will be excluded from this study:
• Evidence of clinically significant cardiovascular, hepatic, gastrointestinal, renal, respiratory, endocrine, hematological, neurological, or psychiatric disease or abnormalities or a known history of any gastrointestinal surgery that could impact the pharmacokinetics of study drug.
• Clinically significant illness within 8 weeks or a clinically significant infection within 4 weeks of dosing.
• Evidence of organ dysfunction or any clinically significant deviation from normal in their medical history.
• Evidence of clinically significant deviation from normal in physical examination, vital signs, or clinical laboratory determinations at Screening or Baseline.
• An interval corrected for heart rate (QTcF) interval greater than 450 msec at Screening or Baseline.
• Females who are either pregnant or lactating.
• A known or suspected history of drug or alcohol abuse within 6 months prior to screening, or who have a positive urine drug test or alcohol test at Screening or Baseline.
• Positive results for Hepatitis B surface antigen (HBsAg) or Hepatitis C antibody (HCV) screen.
• Diagnosis of acquired immune deficiency syndrome (AIDS), or positive test for human immunodeficiency virus (HIV).
• Participation in another clinical trial less than 4 weeks prior to dosing or current enrollment in another clinical trial.
• Receipt of blood products within 4 weeks, or donation of blood within 8 weeks, or donation of plasma within 1 week prior to dosing.
• Hemoglobin level less than 12.0 g/dL.
• Known history of any significant drug or food allergy or an ongoing seasonal allergy.
• Use of prescription drugs within 2 weeks prior to Screening (unless drug has a long t1/2, ie, 5 x t1/2 exceeds 2 weeks).

Sponsors & Collaborators

• Eisai Limited: lead

Study Sites (1)

Unknown Facility

Zuidlarne, Netherlands

Location

MeSH Terms

Interventions

N-(2-fluoro-4-((2-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)carbonylaminopyridin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Study Design

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

Study Record Dates

• First Submitted: August 24, 2015
• First Posted: August 26, 2015
• Study Start: November 1, 2010
• Primary Completion: December 1, 2010
• Study Completion: February 1, 2011
• Last Updated: November 20, 2015

Record last verified: 2015-11

Locations

NL (1)