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Pharmacokinetic Interaction Study of Steady-state Tipranavir/Ritonavir (TPV/r) With Single-dose Valaciclovir (VAL) in Healthy Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02226978
Lead Sponsor
Boehringer Ingelheim
Brief Summary

Assessment of the interaction of tipranavir/ritonavir (TPV/RTV) and valaciclovir (VAL), a prodrug of aciclovir (ACV)

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
29
Inclusion Criteria
  • Healthy male and non-pregnant, non-lactating female subjects as determined by results of screening
  • Signed written informed consent in accordance with Good Clinical Practice (GCP) and local legislation
  • The ability to understand and sign a written informed consent form, prior to participation in any screening procedures and willingness to comply with all study requirements
  • Age >19 and <59 years (20 - 58 years inclusive)
  • Weight ≥ 60 kg
  • Body mass index (BMI) >18.5 and <29.9 kg/m2
Exclusion Criteria
  • Any finding of the medical examination (including blood pressure, pulse rate, and electrocardiogram) deviating from normal and of clinical relevance
  • Atrioventricular (AV) block including 1°
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hematological, oncological or hormonal disorders
  • Surgery of gastrointestinal tract (except appendectomy)
  • Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
  • Relevant history of orthostatic hypotension, fainting spells or blackouts
  • Chronic or relevant acute infections
  • History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
  • Known hypersensitivity to TPV, RTV, valaciclovir, aciclovir or antiretroviral drugs (marketed or experimental use as part of clinical research studies)
  • Known elevated liver enzymes in past trials with any compound
  • Intake of drugs with a long half-life (>24 hours) (<1 month prior to administration)
  • Prescription or over the counter medications (including vitamins, minerals, herbal supplements and antacids), dietary supplements 14 days prior to study drug administration or expected during the trial)
  • Participation in another trial with an investigational drug (<2 months prior to administration or expected during trial)
  • Smoker with a consumption of >10 cigarettes or >3 cigars or >3 pipes/day and those who cannot keep tobacco intake constant
  • Alcohol (>40 g/day for males and >20 g/day for females) and drug abuse
  • Blood donation or loss >400 mL, < 3 month prior to administration
  • Clinically relevant laboratory abnormalities
  • Transaminases above reference values in the history
  • Inability to comply with dietary regimen of study centre

For female subjects:

  • Pregnancy or planning to become pregnant within 60 days of study completion
  • Positive pregnancy test
  • Have not been using a barrier method of contraception for at least 3 months prior to participation in the study if of childbearing potential and not surgically sterilized
  • Are not willing or are unable to use a reliable method of barrier contraception (such as diaphragm with spermicidal cream/jelly or condoms with spermicidal foam), during and up to 2 months after completion/termination of the trial if of childbearing potential and not surgically sterilized
  • Chronic use of oral contraception or hormone replacement containing ethinyl estradiol
  • Breast-feeding

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
TPV/r with valaciclovirValaciclovirVAL 2 days (on days 1 and 13), TPV/r 12 days (on days 2 to 13)
TPV/r with valaciclovirTipranavirVAL 2 days (on days 1 and 13), TPV/r 12 days (on days 2 to 13)
TPV/r with valaciclovirRitonavirVAL 2 days (on days 1 and 13), TPV/r 12 days (on days 2 to 13)
Primary Outcome Measures
NameTimeMethod
Area under the concentration-time curve of aciclovir in plasma over the time interval t0h to t12h (AUC0-12)up to 12 hours after drug administration
Maximum measured concentration of aciclovir in plasma (Cmax)up to 12 hours after drug administration
Secondary Outcome Measures
NameTimeMethod
AUC0-12 for Tipranavir (TPV)up to 12 hours after drug administration
Cmax for TPVup to 12 hours after drug administration
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F)up to 12 hours after drug administration
Terminal half-life of the analyte in plasma (t1/2)up to 12 hours after drug administration
Number of subjects with adverse eventsup to 14 days after last drug administration
Number of subjects with clinically significant findings in laboratory testsup to 14 days after last drug administration
AUC0-12 for Ritonavir (RTV)up to 12 hours after drug administration
Cmax for RTVup to 12 hours after drug administration
Drug concentration of RTV in plasma at 12 hours after administration (C12h)up to 12 hours after drug administration
Drug concentration of TPV in plasma at 12 hours after administration (C12h)up to 12 hours after drug administration
Apparent clearance of the analyte in the plasma after extravascular administration (CL/F)up to 12 hours after drug administration
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