Early Phase 1
N=16
Pharmacokinetic Drug-Drug Interaction Study to Identify Biomarkers of Kidney Transporters
Interaction · Endogenous Biomarkers
Bottom Line
View on ClinicalTrials.gov: NCT05365451 ↗Enrolled (actual)
16
Serious AEs
0.0%
Results posted
Aug 2025
Primary outcome: Primary: Metformin Area Under the Concentration vs. Time Curve (AUC) — 830 mcg*h/L
Study Design & Population
- Study type
- Interventional
- Phase
- Early Phase 1
- Interventions
- MetFORMIN Oral Solution (Drug); Cimetidine 400 MG (Drug); Furosemide Oral Liquid Product (Drug); Probenecid 500 MG (Drug)
- Age
- Adult, Older Adult · 18+ yrs
- Sex
- All
- Sponsor
- Washington State University
- Primary completion
- Jul 2023
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Metformin Area Under the Concentration vs. Time Curve (AUC) |
830 | — |
| PRIMARY Metformin AUC in Presence of Cimetidine |
1030 | — |
| PRIMARY Metformin Maximum Concentration (Cmax) |
124 | — |
| PRIMARY Metformin Cmax in Presence of Cimetidine |
168 | — |
| PRIMARY Metformin Renal Clearance (CLr) |
31 | — |
| PRIMARY Metformin CLr in Presence of Cimetidine |
28 | — |
| PRIMARY Furosemide Area Under the Concentration vs. Time Curve (AUC) |
462.4 | — |
| PRIMARY Furosemide AUC in Presence of Probenecid |
854.6 | — |
| PRIMARY Furosemide Renal Clearance (CLr) |
96.1 | — |
| PRIMARY Furosemide CLr in Presence of Probenecid |
33.4 | — |
Summary
The objective of this study is to confirm the feasibility of using a panel of endogenous substrates/metabolites as a robust biomarker of OCTs and OATs by conducting a controlled, comprehensive clinical drug-drug interaction study in healthy adult volunteers. Metformin and furosemide will be used as probe drugs for OCTs and OATs, respectively; cimetidine and probenecid will be used as corresponding inhibitors. Results from this study will validate this novel approach, which will be extended to children by collaborators at Children's Mercy Hospital in Kansas City, MO.
Eligibility Criteria
Inclusion Criteria
Are from 18-65 years old and healthy
- Are not taking any medications (prescription and non-prescription) or dietary/herbal supplements that can interfere with your ability to eliminate the study drugs from your body
- Are willing to stop taking dietary/herbal supplements and citrus juices for several weeks
- Are willing to stop consuming caffeinated beverages or other caffeine-containing products the evening before and the morning of the first day of each study arm
- Are willing to stop drinking alcoholic beverages for at least 1 day prior to any study day and during the study day
- Are willing to use an acceptable method of birth control that does not include oral contraceptive pills or patches (such as abstinence, copper IUD, condom) throughout your participation in the study and for at least 3 weeks after you last take the study drugs
- Have the time to participate
Exclusion Criteria
- Are under 18 or over 65 years old
- Smoke/vape/chew tobacco products
- Use cannabis products, including marijuana, hemp, and other THC- and CBDcontaining products• Are taking medications or dietary/herbal supplements that can interfere with your ability to eliminate the study drugs from your body
- Have a chronic illness such as (but not limited to) kidney disease, liver disease, diabetes mellitus, high blood pressure, coronary artery disease, chronic obstructive pulmonary disease, cancer, or HIV/AIDS
- Have a hematologic (blood) disorder
- Have a history of drug or alcohol addiction or major psychiatric illness
- Have a history of allergy to metformin, cimetidine, furosemide, or probenecid
- Are pregnant, nursing, or plan to become pregnant within 3 weeks after participation
Data sourced from ClinicalTrials.gov (NCT05365451). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.