Comment Period Extended to 3/23/2015 for Notice of Proposed Rulemaking (NPRM) for FDAAA 801 and NIH Draft Reporting Policy for NIH-Funded Trials

Drug Drug Interaction of BI 201335 and Tenofovir

This study has been completed.
Information provided by (Responsible Party):
Boehringer Ingelheim Identifier:
First received: April 20, 2011
Last updated: November 16, 2011
Last verified: November 2011

The objective of this study is to evaluate the drug-drug interaction potential between BI 201335 and concomitantly administered tenofovir which is used in treatment regimens for HIV infection and/or Hepatitis B infection. Results of this study will serve as a basis for guidance of dose adjustments or other precautionary measures when BI201335 and tenofovir are coadministered.

Condition Intervention Phase
HIV Infections
Drug: tenofovir/BI 201335
Phase 1

Study Type: Interventional
Study Design: Allocation: Non-Randomized
Endpoint Classification: Safety Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: Effect of Multiple Dosing With 240 mg BID BI 201335 on the Steady State Pharmacokinetics of 300mg QD Tenofovir and Effect of Multiple Dosing With 300mg QD Tenofovir on Steady State BI 201335 Pharmacokinetics in Healthy Male and Female Volunteers

Resource links provided by NLM:

Further study details as provided by Boehringer Ingelheim:

Primary Outcome Measures:
  • Comparison of steady-state pharmacokinetics of AUC0-24 of tenofovir on Day 7 with Day 15 [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]
  • Comparison steady-state pharmacokinetics of AUC0-12 of BI 201335 on Day 15 and on Day 22. [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]
  • Comparison of steady-state pharmacokinetics of Cmax of tenofovir on Day 7 with Day 15 [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]
  • Comparison of steady-state pharmacokinetics of C24hr of tenofovir on Day 7 with Day 15 [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]
  • Comparison of steady-state pharmacokinetics of Cmax of BI 201335 on Day 15 and Day22 [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]
  • Comparison of steady-state pharmacokinetics of C12hr of BI 201335 on Day 15 and Day 22 [ Time Frame: 2 weeks ] [ Designated as safety issue: No ]

Secondary Outcome Measures:
  • Number of adverse events during the trial [ Time Frame: approximately 4 weeks ] [ Designated as safety issue: No ]
  • Intensity of adverse events during the trial [ Time Frame: approximately 4 weeks ] [ Designated as safety issue: No ]

Enrollment: 16
Study Start Date: April 2011
Primary Completion Date: June 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: sequence 1
tenofovir medium dose once daily (qd) for first 15 days; BI 201335 medium dose twice daily (bid) on days 8 through day 22 (morning dose on day 22 only)
Drug: tenofovir/BI 201335
tenofovir medium dose once daily (qd) for first 15 days; BI 201335 medium dose twice daily (bid) on days 8 through 22 with last dose on morning of day 22


Ages Eligible for Study:   18 Years to 55 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes

Inclusion criteria:

  1. Healthy males and female subjects and according to medical history, including the physical examination, vital signs (blood pressure, pulse rate), 12-lead electrocardiogram and clinical laboratory tests; all with acceptable findings.
  2. Age =18 to =55 years
  3. Weighing at least 50 kg, and body mass index >=18.5 and BMI <=29.9 kg/m2 (Body Mass Index).
  4. Volunteers must not leave the research unit, during the entire length of the study and must be willing to comply with the protocol and complete all study-related activities.

Exclusion criteria:

  1. Any finding of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance, as assessed by the investigator.
  2. Active diseases of the gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, musculoskeletal, immunologic, rheumatologic, hormonal, neurological system, clinically relevant electrolyte disorders or bleeding disorders that require current medical treatment.
  3. Diseases of the central nervous system or psychiatric disorders.
  4. History of photosensitivity or recurrent rash.
  5. History of orthostatic hypotension, fainting spells or blackouts.
  6. Chronic or clinically relevant acute infections.
  7. History of allergy/hypersensitivity (including drug allergy) which is deemed relevant.
  8. Intake of drugs with a long half-life >24:00 hours within at least one month or less than ten half lives of the respective drug before enrollment in the study (with the exception of hormonal contraceptives).
  9. Use of any drugs which might influence the results of the trial up to 7 days prior to enrolment as nutraceuticals and herbal remedies that would interfere with either the absorption, distribution or metabolism of BI 201335 NA, or that prolong the QT/QTc interval.
  10. Use of any investigational drug within 30 days prior to enrollment; or the planned use of any investigational drug during the course of the current study.
  11. Smoking (>10 cigarettes or >3 cigars or >3 pipes/day)
  12. Inability to abstain from smoking more than 3 cigarettes/day during the period of dosing with study medication.
  13. Drug and alcohol abuse (>60g/day).
  14. Blood donation (more than 100 mL within four weeks prior to administration or during the trial).
  15. Excessive physical activities within one week prior to administration or during the trial.
  16. Any laboratory value outside the reference range that is of clinical relevance at screening, according to the judgment of the investigator, and in consultation with the clinical monitor.
  17. Known elevated liver enzymes in past with any compound (experimental or marketed).
  18. Concomitant administration of any food product known to alter P450 enzyme activity such as grapefruit juice, Seville oranges, St. John's Wort.
  19. Concomitant administration of oral contraceptives (subjects who stopped oral contraceptives at least 7 days prior to Day 1 may be included.
  20. Inadequate venous access.
  21. A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTcF, or QTcB interval >450 ms).
  22. Infection with hepatitis B (HBV), or hepatitis C virus (HCV),
  23. Positive test for HIV-1 or HIV-2. For women of child bearing potential (WOCBP)
  24. Pregnancy or planning to become pregnant within 2 months of study completion
  25. Positive pregnancy test at screening visit
  26. No proof of sterilization, or not willing or unable to consistently use an acceptable method of double barrier contraception including IUD, or diaphragm with spermicidal cream/jelly and condoms for male partner, during and up to 3 months after completion/termination of the trial.
  27. Lactation period with active breastfeeding from time of screening to 30 days after end of trial visit.

    For male subjects

  28. No proof of sterilization, or not willing or unable to consistently use an acceptable method of double barrier contraception including a condom each time and female partner of child bearing potential consistently uses oral birth control pills, or an IUD, or a diaphragm with spermicidal cream/jelly). Male subjects must not father a child from administration of the first dose and up to 3 months after the last dose of study medication.
  Contacts and Locations
Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its identifier: NCT01340196

United States, New York
1220.50.0001 Boehringer Ingelheim Investigational Site
Buffalo, New York, United States
Sponsors and Collaborators
Boehringer Ingelheim
Study Chair: Boehringer Ingelheim Boehringer Ingelheim
  More Information

No publications provided

Responsible Party: Boehringer Ingelheim Identifier: NCT01340196     History of Changes
Other Study ID Numbers: 1220.50
Study First Received: April 20, 2011
Last Updated: November 16, 2011
Health Authority: United States: Food and Drug Administration

Additional relevant MeSH terms:
Tenofovir disoproxil
Anti-HIV Agents
Anti-Infective Agents
Anti-Retroviral Agents
Antiviral Agents
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Nucleic Acid Synthesis Inhibitors
Pharmacologic Actions
Reverse Transcriptase Inhibitors
Therapeutic Uses processed this record on March 01, 2015