Efavirenz and Ritonavir on Human Brain P-Glycoprotein

Phase 1

Completed

• Conditions: Drug Effects
• Interventions: Drug: [11C] desmethyl-loperamide; Other: Control - no pretreatment; Drug: Oral ritonavir; Drug: Oral efavirenz

• Registration Number: NCT01668147
• Lead Sponsor: Washington University School of Medicine

Brief Summary

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

Detailed 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

Basic Information
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Recruitment & Eligibility
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Study & Design
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Trial Locations

Study Timeline

• Study First Submitted: 2012-07-30
• Study Start: 2012-08
• Study First Submitted QC: 2012-08-15
• Study First Posted: 2012-08-17
• Primary Completion: 2016-06
• Study Completion: 2016-08
• Results First Submitted: 2018-06-21
• Status Verified: 2020-01
• Results First Submitted QC: 2020-01-08
• Last Update Submitted: 2020-01-08
• Results First Posted: 2020-01-22
• Last Update Posted: 2020-01-22

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 13

Inclusion Criteria

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

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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

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Control	[11C] desmethyl-loperamide	Session 1: Control (no pretreatment) - IV 10-14 mCi of \[11C\] desmethyl-loperamide (dLop) with PET/CT imaging
Control	Control - no pretreatment	Session 1: Control (no pretreatment) - IV 10-14 mCi of \[11C\] desmethyl-loperamide (dLop) with PET/CT imaging
Oral ritonavir	[11C] desmethyl-loperamide	Session 2: Pretreatment with oral ritonavir for 3 days followed by IV 10-14 mCi of \[11C\]dLop with PET/CT imaging
Oral ritonavir	Oral ritonavir	Session 2: Pretreatment with oral ritonavir for 3 days followed by IV 10-14 mCi of \[11C\]dLop with PET/CT imaging
Oral efavirenz	[11C] desmethyl-loperamide	Session 3: Pretreatment with oral efavirenz for 14 days followed by IV 10-14 mCi of \[11C\]dLop with PET/CT imaging
Oral efavirenz	Oral efavirenz	Session 3: Pretreatment with oral efavirenz for 14 days followed by IV 10-14 mCi of \[11C\]dLop with PET/CT imaging

Primary Outcome Measures

Name	Time	Method
Cerebral [11C]dLop Distribution Volume	1 day

Trial Locations

Locations (1)

Washington University School of Medicine; 🇺🇸 Saint Louis, Missouri, United States