Efavirenz and Ritonavir on Human Brain P-Glycoprotein

Drug Effects Clinical Trial

Official title:

Influence of Efavirenz and Ritonavir on Human Brain P-Glycoprotein Activity Using PET Imaging

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT01668147
• Other study ID #: 201205135
• Status: Completed
• Phase: Phase 1/Phase 2
• Start date: August 2012
• Est. completion date: August 2016

Study information

• Verified date: January 2020
• Source: Washington University School of Medicine
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial Summary

To determine the effects of ritonavir and efavirenz on the activity of P-glycoprotein in human brain.

Description:

Sequential crossover using tracer 11C-desmethylloperamide, a substrate for brain P-glycoprotein, and positron emission tomography (PET), administered after nothing (control), oral ritonavir (3d), and oral efavirenz (14d) with washout in between

Recruitment information / eligibility

• Status: Completed
• Enrollment: 13
• Est. completion date: August 2016
• Est. primary completion date: June 2016
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: All
• Age group: 18 Years to 40 Years

Eligibility

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

Related Conditions & MeSH terms

• Drug Effects

Intervention

Drug:
• [11C] desmethyl-loperamide
IV administration of 10-14 mCi of [11C] desmethyl-loperamide with PET/CT imaging

Other:
• Control - no pretreatment
Session 1: IV administration of 10-14 mCi [11C] desmethyl-loperamide (dLop) with PET/CT imaging and brain MRI

Drug:
• Oral ritonavir
Session 2: Pretreatment with oral ritonavir for 3 days followed by IV administration of 10-14 mCi [11C]dLop with PET/CT imaging and brain MRI
• Oral efavirenz
Session 3: Pretreatment with oral efavirenz for 14 days followed by IV administration of 10-14 mCi [11C]dLop with PET/CT imaging and brain MRI

Locations

Country	Name	City	State
United States	Washington University School of Medicine	Saint Louis	Missouri

Sponsors (1)

Lead Sponsor	Collaborator
Washington University School of Medicine

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Cerebral [11C]dLop Distribution Volume		1 day