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Clinical Evaluation of Adjusted Doses of Darunavir/Ritonavir With Rifampicin in HIV-infected Volunteers

Phase 1
Terminated
Conditions
HIV Infections
Interventions
Drug: Darunavir/ritonavir 800/100 mg tablet
Registration Number
NCT03892161
Lead Sponsor
University of Cape Town
Brief Summary

The DaRifi study aims:

1. Develop adjusted doses of darunavir/ritonavir for use in HIV-infected patients requiring co-treatment of TB with a rifampicin-based regimen.

2. Compare the steady state pharmacokinetics of doubled doses of DRV/r with rifampicin (in once daily and 12-hourly approaches) to standard daily doses without rifampicin.

3. Twenty-eight volunteers will be enrolled for a target of 24 participants completing the study.

Detailed Description

A significant barrier to the use of better tolerated antiretrovirals in many low-to-middle income countries (LMIC), where tuberculosis (TB) is endemic, is a lack of evidence to support their use in patients with TB. Access to optimal protease inhibitor (PI)-based regimens for patients with and without TB is urgent. Switching rifampicin to rifabutin, a weak inducer that does not significantly reduce PI concentrations, is recommended in high income countries for patients on boosted PIs who develop TB. However, rifabutin is not available in most LMIC where TB is typically treated with fixed dose combination tablets.

We will enrol virologically suppressed participants on a second-line DRV/r regimen without TB. Based on data from a Physiologically-Based PK model, we selected two adjusted doses of DRV/r (1600/200 mg daily and 800/100 mg 12 hourly) with RIF for comparison to plasma exposures with DRV/r 800/100 mg daily without RIF, in a cross-over design.

Baseline DRV steady state PK will be determined and RIF added for 7 days, then the dose of ritonavir will be increased to 200 mg; 7 days later the dose of DRV will be increased; after another 7 days participants will be crossed over to the alternative adjusted DRV dose.

DRV will be measured in plasma samples after observed doses at baseline and after each dose adjustment. Non-compartmental analysis will be used to estimate the PK measures. Clinical adverse events, ALT, and bilirubin will be monitored every 2 to 3 days during treatment with RIF.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
17
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Standard DRV/r with RifampicinRifampicin 600mg QD tablet and DTG 50mg BDRifampicin 600mg QD will be added and darunavir/ritonavir steady state pharmacokinetic analysis will be performed.
Boosed ritonavir 200mgRifampicin 600mg QD tablet and DTG 50mg BDRifampicin 600mg QD continued with ritonavir 200mg dose doubled QD and darunavir remains 800mg QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Double dose DRV/r 1600/200mg QDRifampicin 600mg QD tablet and DTG 50mg BDRifampicin 600mg QD and DTG QD continued. Double dose DRV/r QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Double dose DRV/r 800/100mg BDRifampicin 600mg QD tablet and DTG 50mg BDRifampicin 600mg QD and DTG BD continued. Double dose DRV/r QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Boosed ritonavir 200mgDarunavir/ritonavir 800/100 mg tabletRifampicin 600mg QD continued with ritonavir 200mg dose doubled QD and darunavir remains 800mg QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Standard dose DRV/rDarunavir/ritonavir 800/100 mg tabletStandard dose DRV/r 800/100mg without Rifampicin
Double dose DRV/r 1600/200mg QDDarunavir/ritonavir 800/100 mg tabletRifampicin 600mg QD and DTG QD continued. Double dose DRV/r QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Standard DRV/r with RifampicinDarunavir/ritonavir 800/100 mg tabletRifampicin 600mg QD will be added and darunavir/ritonavir steady state pharmacokinetic analysis will be performed.
Double dose DRV/r 800/100mg BDDarunavir/ritonavir 800/100 mg tabletRifampicin 600mg QD and DTG BD continued. Double dose DRV/r QD. The darunavir/ritonavir steady state pharmacokinetic analysis will be performed and compared.
Primary Outcome Measures
NameTimeMethod
Darunavir plasma concentrations nanogram per milliliter (ng/ml)1 year

Darunavir plasma concentrations will be compared with rifampicin and without rifampicin.

Secondary Outcome Measures
NameTimeMethod
Alanine Transaminase (ALT) blood level (iu/L)1 Year

Clinical safety will be monitored, ALT liver enzyme tests will be evaluated every 3 days.

Trial Locations

Locations (1)

Clinical Research Centre

🇿🇦

Cape Town, Western Cape, South Africa

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