Randomized, Placebo-controlled Study to Evaluate Effects of E5555 on Renal Function Parameters and OCT2 Activity

Eisai Inc.104 enrolled

Overview

This is a drug-drug interaction study to evaluate the effects of steady-state exposure of E5555 and its main metabolites on the pharmacokinetics (PK) of metformin, an organic cation transporter-2 (OCT2) substrate. In addition, the study will also investigate the effects of E5555 on several renal function parameters.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

QUADRUPLE

Enrollment

104

Conditions

Healthy Subjects

Interventions

E5555DRUG

Drug: Oral E5555 400 mg/matching placebo, oral metformin 500 mg, iohexal 20 mL intravenous (IV), and para-aminohippuric acid (PAH) 7 mg/kg IV.

E5555DRUG

Drug: Oral E5555 100 mg/matching placebo, oral metformin 500 mg, iohexal 20 mL intravenous (IV), and para-aminohippuric acid (PAH) 7 mg/kg IV bolus.

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: \- Healthy male or female subjects aged greater than or equal to 18 years to 55 years Exclusion Criteria: * History of any medical condition which will result in an increased risk of bleeding including but not limited to active or recurrent gastric ulcers, recent head trauma or surgery, severe hypertension, bacterial endocarditis, etc. * Creatinine clearance \< 90 mL/min as estimated using Cockcroft-Gault formula at screening or baseline * History of any renal disorders, proteinuria, hepato-biliary disease.

Locations (1)

Quintiles Phase I Services

Overland Park, Kansas, United States

Outcomes

Primary Outcomes

To evaluate the effects of multiple doses of E5555 on single dose pharmacokinetics of metformin.

Time frame: 15 days

Secondary Outcomes

To assess the effects of multiple doses of E5555 on the glomerular filtration rate estimated using iohexol.

Time frame: Days 7 and 14

To assess the effects of multiple doses of E5555 on the effective renal plasma flow estimated using para-aminohippuric acid (PAH).

Time frame: Days 7 and 14

To assess the multiple dose pharmacokinetics of E5555 and its main 6 metabolites.

Time frame: Days 12-18

To assess the safety and tolerability of multiple doses of E5555 and a single dose of metformin either given alone or concomitantly

Time frame: Day 1 - Day 18

Data from ClinicalTrials.gov

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