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Phase 2 Completed N=50 Randomized Treatment

TMC125-TiDP2-C238: An Exploratory Pharmacokinetics, Safety and Anti-HIV Activity Study of Etravirine (ETR) When Given With Boosted Atazanavir (ATV/Rtv) at Two Different Doses and 1 Nucleoside Reverse Transcriptase Inhibitor (NRTI) in Treatment Experienced HIV Patients

HIV · Acquired Immunodeficiency Syndrome
Source: ClinicalTrials.gov NCT00896051 ↗
Enrolled (actual)
50
Serious AEs
12.0%
Results posted
Sep 2013
Primary outcomePrimary: Pharmacokinetic Results of Atazanavir (ATV): Treatment A: ATV/Low-Dose Ritonavir (Rtv) 300/100 mg (Results for C0h, Cmin, and Cmax) — 1339; 845.7; 1104; 758.6 ng/ml

Summary

The purpose of this study is to determine the pharmacokinetics (how the body absorbs, distributes, metabolizes and eliminates a drug) (PK) of ETR when given with ATV/rtv and 1 NRTI in treatment experienced HIV-1 infected patients. In addition, safety, tolerability and anti-HIV effect of this regimen will also be studied. A total of 46 patients will be enrolled.

Outcome Measures

OutcomeResultp-value
PRIMARY
Pharmacokinetic Results of Atazanavir (ATV): Treatment A: ATV/Low-Dose Ritonavir (Rtv) 300/100 mg (Results for C0h, Cmin, and Cmax)
1339; 845.7; 1104; 758.6; 5652; 5232
PRIMARY
Pharmacokinetic Results of Atazanavir (ATV): Treatment A: ATV/Low-Dose Ritonavir (Rtv) 300/100 mg (Results for AUC24hr)
60030; 55070
PRIMARY
Pharmacokinetic Results of Atazanavir (ATV): Treatment B: ATV/Low-Dose Ritonavir (Rtv) 400/100 mg (Results for C0h, Cmin, and Cmax)
1898; 1545; 1671; 1107; 6419; 6950
PRIMARY
Pharmacokinetic Results of Atazanavir (ATV): Treatment B: ATV/Low-Dose Ritonavir (Rtv) 400/100 mg (Results for AUC24hr)
74210; 72220
PRIMARY
Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment A: Atazanavir (ATV)/Rtv 300/100 mg (Results for C0h, Cmin, and Cmax)
143.4; 102.5; 60.42; 43.97; 1834; 1740
PRIMARY
Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment A: Atazanavir (ATV)/Rtv 300/100 mg (Results for AUC24hr)
12560; 11120
PRIMARY
Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment B: Atazanavir (ATV)/Rtv 400/100 mg (Results for C0h, Cmin, and Cmax)
109.2; 163.4; 64.70; 75.68; 1882; 1847
PRIMARY
Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment B: Atazanavir (ATV)/Rtv 400/100 mg (Results for AUC24hr)
13880; 13660
PRIMARY
Pharmacokinetic Results of Etravirine (ETR) (Results for C0h, Cmin, and Cmax)
422.2; 316.6; 425.1; 286.5; 773.0; 628.7
PRIMARY
Pharmacokinetic Results of Etravirine (ETR) (Results for AUC12hr)
7629; 5171
PRIMARY
Percentage of Participants With Undetectable Plasma Viral Load (VL) Values (<50 Copies/mL) at Week 48
50.0; 45.5
SECONDARY
Change From Prebaseline in CD4+ Cell Count Over Time
16; 8; 55; 46; 31; 72
SECONDARY
The Percentage of Participants With a Virologic Response Using the Non-Completing = Failure (NC=F) Imputation Method
9.1; 9.1; 31.8; 36.4; 59.1; 59.1
SECONDARY
The Percentage of Participants With a Virologic Response Using the Time to Loss of Virologic Response (TLOVR) Imputation Method
9.1; 4.5; 31.8; 36.4; 59.1; 54.5
SECONDARY
The Percentage of Participants With a Virologic Response (Plasma Viral Load < 50 Copies/mL) at Week 48 Using the Snapshot Analysis Method
50.0; 45.5; 31.8; 36.4; 18.2; 18.2
SECONDARY
Change From Pre-Baseline in Log10 Viral Load Over Time
-1.4; -1.4; -1.9; -1.8; -1.7; -2.0
SECONDARY
Time to Confirmed Virologic Response
71.0; 76.0; 28.0; 28.0
SECONDARY
Time to Virologic Failure
318.0; NA; NA; NA

Eligibility Criteria

Inclusion Criteria

  • Documented HIV-1 infection
  • Failing on a stable ART (anti retroviral therapy) with HIV-1 plasma viral load above 500 HIV-1 RNA copies/ml
  • Presence of at least 1 documented NNRTI mutation
  • Demonstrated sensitivity to ATV, ETR and at least one of the selected NRTIs based on the resistance test at screening
  • General medical condition, in the investigator's opinion, does not interfere with the assessments and completion of the trial
  • Substudy: patients who have been treated in C238 for more than 24 weeks and are currently suppressed (defined as patients with at least 2 most recent and consecutive viral loads less than 50 cp/mL) will be considered eligible for the substudy

Exclusion Criteria

  • Primary HIV-1 infection
  • Previously documented HIV-2 infection
  • Previously failed 2 or more HIV PI-containing regimens
  • Previous diagnosis of hereditary hyperbilirubinemia (eg. Gilbert's syndrome, Crigler-Najjar syndrome).

Grade 3 or 4 toxicities (according to DAIDS grading)

  • Acute and chronic viral hepatitis
  • Receipt of an investigational drug or investigational vaccine within 30 days prior to the trial drug administration
  • Pregnant or breastfeeding female
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT00896051). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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