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

This study has been completed.
Information provided by (Responsible Party):
Eisai Inc. Identifier:
First received: November 15, 2010
Last updated: July 10, 2014
Last verified: July 2014
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.

Condition Intervention Phase
Healthy Subjects
Drug: E5555
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: Double Blind (Participant, Care Provider, Investigator, Outcomes Assessor)
Primary Purpose: Treatment
Official Title: A Single-center, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Effects of Multiple Doses of E5555 on the Pharmacokinetics of Metformin (a Substrate for OCT2 Transporter) and on Renal Function in Healthy Subjects

Resource links provided by NLM:

Further study details as provided by Eisai Inc.:

Primary Outcome Measures:
  • To evaluate the effects of multiple doses of E5555 on single dose pharmacokinetics of metformin. [ Time Frame: 15 days ]

Secondary Outcome Measures:
  • 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 ]

Enrollment: 104
Study Start Date: October 2010
Primary Completion Date: August 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Arm 1 Drug: E5555
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.
Experimental: Arm 2 Drug: E5555
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.


Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

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.
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Please refer to this study by its identifier: NCT01241669

United States, Kansas
Quintiles Phase I Services
Overland Park, Kansas, United States, 661200
Sponsors and Collaborators
Eisai Inc.
Study Director: Dr. Bhaskar Rege Eisai Inc.
  More Information

Responsible Party: Eisai Inc. Identifier: NCT01241669     History of Changes
Other Study ID Numbers: E5555-A001-023
Study First Received: November 15, 2010
Last Updated: July 10, 2014

Additional relevant MeSH terms:
Hypoglycemic Agents
Physiological Effects of Drugs processed this record on May 25, 2017