Efavirenz and Ritonavir on Human Brian P-Glycoprotein (dLOP)

This study is ongoing, but not recruiting participants.
Sponsor:
Information provided by (Responsible Party):
Washington University School of Medicine
ClinicalTrials.gov Identifier:
NCT01668147
First received: July 30, 2012
Last updated: December 9, 2013
Last verified: December 2013
  Purpose

The purpose of this research study is to determine the effects of ritonavir and efavirenz on the activity of P-glycoprotein in human brain.

Screening

Health self-assessment and undergo a medical history and physical examination, including a structured interview to screen for history of medical conditions, fasting blood glucose and HIV blood tests, urine HCG pregnancy test for women of childbearing potential will be performed within 24hr of study drug administration

Study visits Subjects will be studied on three occasions, with a washout between sessions. Sessions 1: Control (no pretreatment) - intravenous administration of 10 - 14 mCi of [11C] desmethyl-loperamide (dLop) with PET/CT imaging Session 2: Pretreatment with oral ritonavir for 3 days followed by intravenous administration of 10 - 14 mCi of [11C]dLOP with PET/CT imaging Session3: Pretreatment with oral efavirenz for 14 days followed by intravenous administration of 10 - 14 mCi of [11C]dLOP with PET/CT imaging


Condition Intervention
Drug Effects
Drug: [11c] desmethyl-loperamide (dLop)
Drug: Ritonavir
Drug: Efavirenz

Study Type: Interventional
Study Design: Intervention Model: Single Group Assignment
Masking: Open Label
Official Title: Influence of Efavirenz and Ritonavir on Human Brain P-Glycoprotein Activity Using PET Imaging

Resource links provided by NLM:


Further study details as provided by Washington University School of Medicine:

Primary Outcome Measures:
  • cerebral [11C]dLop distribution volume [ Time Frame: approximately 3 months ] [ Designated as safety issue: No ]
    blood tests and PET data analysis and interpretation.


Estimated Enrollment: 8
Study Start Date: August 2012
Estimated Study Completion Date: August 2016
Estimated Primary Completion Date: June 2014 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: study arm
Sessions 1: Control (no pretreatment) - intravenous administration of 10-14 mCi of [11C] desmethyl-loperamide (dLop) with PET/CT imaging Session 2: Pretreatment with oral ritonavir for 3 days followed by intravenous administration of 10-14 mCi of [11C]dLop with PET/CT imaging Session3: Pretreatment with oral efavirenz for 14 days followed by intravenous administration of 10-14 mCi of [11C]dLop with PET/CT imaging
Drug: [11c] desmethyl-loperamide (dLop)
intravenous administration of 10-14 mCi of [11C] desmethyl-loperamide (dLop) with PET/CT imaging
Other Name: DESMETHYL LOPERAMIDE
Drug: Ritonavir
Pretreatment with oral ritonavir for 3 days followed by intravenous administration of 10-14 mCi of [11C]dLop with PET/CT imaging
Other Name: Kaletra
Drug: Efavirenz
Pretreatment with oral efavirenz for 14 days followed by intravenous administration of 10-14 mCi of [11C]dLop with PET/CT imaging
Other Name: Sustiva,Atripla

  Show Detailed Description

  Eligibility

Ages Eligible for Study:   18 Years to 40 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Male or non-pregnant female, 18-40 yr old
  • Good general health with no remarkable medical conditions
  • BMI < 33
  • Provide informed consent

Exclusion Criteria:

  • Known history of liver or kidney disease
  • History of major medical conditions
  • HIV seropositive
  • Fasting blood glucose > 110 mg/dl
  • Family history of type 2 diabetes
  • Use of prescription or non prescription medications, herbals or foods known to be metabolized by or altering P-glycoprotein or CYP3A activity (hormonal birth control medications are acceptable if alternative means of contraception are used)
  • Females who are pregnant or nursing
  • Females taking hormonal contraceptives who are unwilling to use alternative means of contraception
  • Contraindications to MRI
  • Contraindications to PET scanning
  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 ClinicalTrials.gov identifier: NCT01668147

Locations
United States, Missouri
Washington University School of Medicine
St. Louis, Missouri, United States, 63110
Sponsors and Collaborators
Washington University School of Medicine
Investigators
Principal Investigator: Evan Kharasch, MD, PhD. Washington University School of Medicine
  More Information

No publications provided

Responsible Party: Washington University School of Medicine
ClinicalTrials.gov Identifier: NCT01668147     History of Changes
Other Study ID Numbers: 201205135
Study First Received: July 30, 2012
Last Updated: December 9, 2013
Health Authority: United States: Institutional Review Board

Keywords provided by Washington University School of Medicine:
PET Imaging
Efavirenz
Ritonavior
[11C] desmethyl-loperamide
Healthy volunteers

Additional relevant MeSH terms:
Ritonavir
Efavirenz
Loperamide
Antidiarrheals
HIV Protease Inhibitors
Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Pharmacologic Actions
Anti-HIV Agents
Anti-Retroviral Agents
Antiviral Agents
Anti-Infective Agents
Therapeutic Uses
Reverse Transcriptase Inhibitors
Nucleic Acid Synthesis Inhibitors
Gastrointestinal Agents

ClinicalTrials.gov processed this record on September 16, 2014