Healthy VolunteersPhase 1NCT01250535
Human Cytochrome P450 4F Enzymes and Drug Interactions
A Phase 1 study testing Warfarin and Lovastatin in people with Healthy Volunteers and Drug Drug Interactions, run by University of North Carolina, Chapel Hill at 1 site in United States.
Trial summary
Drug-drug interactions play an important role in clinical adverse events due to the prevalence of multi-drug therapy. Co-administration of warfarin and a statin has expanded substantially in the US over the last decades. Read more about this study
- Who is it for?
- Ages 18 to 60 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy Volunteers, Drug Drug Interactions
- What is being tested?
- Warfarin and Lovastatin
- Could I receive a placebo?
- Yes, some participants may receive a placebo
- How many people
- 19 participants
- Where
- 1 siteUnited States
- Study dates
- Dec 2010to Dec 2011
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 60 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Normal baseline clinical laboratory results including coagulation panel (prothrombin time (PT), international normalized ratio (INR), activated partial thromboplastin time (APTT)), liver function tests (ALT, AST, alkaline phosphatase and total bilirubin), kidney function tests (serum creatinine and BUN), lipid panel (cholesterol, LDL-C, HDL-C, and triglycerides), and blood creatine kinase
- Minimum weight of 110 lbs and minimum hemoglobin level at 12.5 g/dL
- Ability to understand the informed consent form
- Willing to abstain from grapefruit products, alcohol, and physical contact sports
Who cannot join
- History of intolerance, allergy, or hypersensitivity to study drugs warfarin and lovastatin or any substances contained in the medication
- History of clotting disorders, stroke, hypertension, anemia, renal insufficiency, hepatic dysfunction, platelet dysfunction, gastrointestinal bleeding, or any recent bleeding episode or trauma within 6 months
- History of significant medical conditions that the study physician believes would increase risk (e.g., additional bleeding disorders)
- Genotype non-homozygous for CYP2C9*1 or genotype VKORC1-1639AA
- History of significant alcohol abuse and/or illicit drug use
- Tobacco use within the month preceding the study
Show all 13Show fewer
- Woman who is pregnant or breastfeeding
- Women who are unable to maintain adequate birth control during the study
- Post-menopausal women on estrogen replacement
- Chronic statin or warfarin use
- Taking concomitant medications, both prescription and non-prescription (including herbal products, over-the-counter medications, and multivitamins), known to alter lovastatin, warfarin, or vitamin K blood levels (women stabilized on hormonal methods of birth control will be allowed to participate, and subjects stabilized on antidepressant medications will be allowed to participate)
- Recent use of antibacterial antibiotics
- Recent blood donation or participation in other clinical studies within past 8 weeks
Trial locations and contacts
1 site in 1 country.
United States1 site
University of North Carolina, Clinical and Translational Research Center (CTRC)
Chapel Hill, North Carolina, 27599
About this study
Drug-drug interactions play an important role in clinical adverse events due to the prevalence of multi-drug therapy. Co-administration of warfarin and a statin has expanded substantially in the US over the last decades. The purpose of this study is to develop a mechanistic understanding of the role of a drug-metabolizing enzyme, CYP4F2, in the interaction between warfarin and statins. This study will test the hypothesis that lovastatin potentiates the anticoagulant effect of warfarin by inducing vitamin K-metabolizing enzyme CYP4F2 in humans, thus increasing warfarin's anticoagulant effect.
- Conditions
- Healthy Volunteers, Drug Drug Interactions
- Being tested
- Warfarin, Placebo, Lovastatin
- Keywords
- Drug drug interactions, Warfarin, Anticoagulants, Lovastatin, Statins, CYP4F2, Vitamin K
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
WarfarinDrug
Also called Coumadin
10 mg, po, single dose on day 7
PlaceboDrug
po, once a day, days 1 through 14
LovastatinDrug
Also called Mevacor
40 mg, po, once a day, days 1 through 14
| Study group | Role | What they receive |
|---|---|---|
| Warfarin plus lovastatin | Experimental | Warfarin plus lovastatin Receives: Drug: Warfarin; Drug: Lovastatin |
| Warfarin plus placebo | Placebo comparator | Warfarin plus placebo Receives: Drug: Warfarin; Drug: Placebo |
What is being measured
The primary outcome is the main question the study is designed to answer.
Pharmacodynamics
Measurement of Prothrombin time (PT) to assess the International Normalized Ratio (INR).
Measured: Measurement will be performed before (baseline) and 2, 4, 8, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168h after co-administration of warfarin and lovastatin/placebo and during screening.
Secondary outcomes (2)
Pharmacokinetics
Vitamin K1 and vitamin K1 metabolite measured by maximum plasma concentration and AUC.
Measured: Sampling will be performed before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168 h after co-administration of warfarin and lovastatin/placebo.
Pharmacokinetics
Pharmacokinetics for (R)- and (S)- Warfarin, and lovastatin measured by maximum plasma concentration and AUC.
Measured: Sampling will be performed before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168 h after co-administration of warfarin and lovastatin/placebo.
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted30 Nov 2010 (estimated)
- Study startDec 2010
- Primary completionDec 2011
- Study completionDec 2011
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Healthy VolunteersStudies of the same condition, open and under way.
- More trials run by University of North Carolina, Chapel HillThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Triple blind
- Who is masked
- Participant, Care provider, Investigator
- Enrolment
- 19 participants (actual)
Sponsor and investigators
- Lead sponsor
- University of North Carolina, Chapel Hill
- Sponsor type
- University, hospital or other
- Collaborators
- National Institutes of Health (NIH)
- Responsible party
- Principal investigator, Kim Brouwer, PharmD, PhD, University of North Carolina, Chapel Hill
- Investigators
- Michael Z Wang, PhD, Study director, University of KansasKim LR Brouwer, PharmD PhD, Principal investigator, University of North Carolina, Chapel Hill
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01250535
- Sponsor's protocol ID
- 10-0576
- Other IDs
- 1R01GM089994-01A1
- Status last verified
- Jan 2013
- First submitted
- 29 Nov 2010
- Last updated
- 21 Jan 2013
- Results posted
- No
- Data monitoring committee
- No
Study at a glance
From the registry record, last updated by the sponsor on 21 Jan 2013. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Human Cytochrome P450 4F Enzymes and Drug Interactions
- ClinicalTrials.gov ID
- NCT01250535
- Acronym / sponsor ID
- 10-0576
- Conditions
- Healthy Volunteers, Drug Drug Interactions
- Keywords
- Drug drug interactions, Warfarin, Anticoagulants, Lovastatin, Statins, CYP4F2, Vitamin K
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 19 participants (actual)
- Lead sponsor
- University of North Carolina, Chapel HillUniversity, hospital or other
- Collaborators
- National Institutes of Health (NIH)
- Study start
- Dec 2010
- Primary completion
- Dec 2011 (actual)
- Study completion
- Dec 2011 (actual)
- First posted
- 30 Nov 2010 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
Drug-drug interactions play an important role in clinical adverse events due to the prevalence of multi-drug therapy. Co-administration of warfarin and a statin has expanded substantially in the US over the last decades. The purpose of this study is to develop a mechanistic understanding of the role of a drug-metabolizing enzyme, CYP4F2, in the interaction between warfarin and statins. This study will test the hypothesis that lovastatin potentiates the anticoagulant effect of warfarin by inducing vitamin K-metabolizing enzyme CYP4F2 in humans, thus increasing warfarin's anticoagulant effect.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Triple blind (participant, care provider, investigator)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| Warfarin plus lovastatin | Experimental | Drug: Warfarin, Drug: LovastatinWarfarin plus lovastatin |
| Warfarin plus placebo | Placebo comparator | Drug: Warfarin, Drug: PlaceboWarfarin plus placebo |
Who may qualify
- Ages
- 18 to 60 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- Normal baseline clinical laboratory results including coagulation panel (prothrombin time (PT), international normalized ratio (INR), activated partial thromboplastin time (APTT)), liver function tests (ALT, AST, alkaline phosphatase and total bilirubin), kidney function tests (serum creatinine and BUN), lipid panel (cholesterol, LDL-C, HDL-C, and triglycerides), and blood creatine kinase
- Minimum weight of 110 lbs and minimum hemoglobin level at 12.5 g/dL
- Ability to understand the informed consent form
- Willing to abstain from grapefruit products, alcohol, and physical contact sports
Key exclusion criteria (13 listed)
- History of intolerance, allergy, or hypersensitivity to study drugs warfarin and lovastatin or any substances contained in the medication
- History of clotting disorders, stroke, hypertension, anemia, renal insufficiency, hepatic dysfunction, platelet dysfunction, gastrointestinal bleeding, or any recent bleeding episode or trauma within 6 months
- History of significant medical conditions that the study physician believes would increase risk (e.g., additional bleeding disorders)
- Genotype non-homozygous for CYP2C9*1 or genotype VKORC1-1639AA
- History of significant alcohol abuse and/or illicit drug use
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| WarfarinAlso: Coumadin10 mg, po, single dose on day 7 | Drug | Warfarin plus lovastatin, Warfarin plus placebo |
| Placebopo, once a day, days 1 through 14 | Drug | Warfarin plus placebo |
| LovastatinAlso: Mevacor40 mg, po, once a day, days 1 through 14 | Drug | Warfarin plus lovastatin |
Primary outcome
Pharmacodynamics
Time frame: Measurement will be performed before (baseline) and 2, 4, 8, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168h after co-administration of warfarin and lovastatin/placebo and during screening.
Measurement of Prothrombin time (PT) to assess the International Normalized Ratio (INR).
2 secondary outcomes
Pharmacokinetics
Time frame: Sampling will be performed before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168 h after co-administration of warfarin and lovastatin/placebo.
Pharmacokinetics
Time frame: Sampling will be performed before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168 h after co-administration of warfarin and lovastatin/placebo.
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 21 Jan 2013.
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Pain
Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Michael Z Wang, PhD study director
University of Kansas
Kim LR Brouwer, PharmD PhD principal investigator
University of North Carolina, Chapel Hill
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Warfarin and Lovastatin in people with Healthy Volunteers and Drug Drug Interactions, run by University of North Carolina, Chapel Hill at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 4 inclusion and 13 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 21 Jan 2013. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. Some participants in this study may receive a placebo. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Pharmacodynamics (time frame: Measurement will be performed before (baseline) and 2, 4, 8, 12, 24, 36, 48, 60, 72, 96, 120, 144, and 168h after co-administration of warfarin and lovastatin/placebo and during screening.). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 21 Jan 2013; AzTrials last refreshed its copy on 6 Nov 2026.