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A Phase 2B Multicenter, Randomized, Comparative Trial Of UK-453,061 Versus Etravirine In Combination With Darunavir/Ritonavir And A Nucleos(t)Ide Reverse Transcriptase Inhibitor For The Treatment Of Antiretroviral Experienced HIV-1 Infected Subjects With Evidence Of NNRTI Resistant HIV-1

Phase 2
Terminated
Conditions
HIV-1
Interventions
Drug: UK-453,061 Dose 2
Drug: UK-453,061 Dose 1
Registration Number
NCT00823979
Lead Sponsor
Pfizer
Brief Summary

This is a 96 week study to determine if UK- 453,061 in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor is as efficacious, safe and tolerable as etravirine in combination with Darunavir /ritonavir and a Nucleos(t)ide Reverse Transcriptase inhibitor in HIV-1 infected patients who have been previously treated with antiretroviral drugs and have NNRTI resistance mutations.

Detailed Description

The trial was terminated on 12 April, 2012 due to lack of efficacy at the Week 24 analysis. The decision to terminate the trial was not based on any safety concerns.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
105
Inclusion Criteria
  • Male or female at least 18 years of age available for a follow-up period of at least 96 weeks.
  • HIV 1 RNA viral load of greater then 500 copies/mL.
  • Negative urine pregnancy test.
Exclusion Criteria
  • Suspected or documented active, untreated HIV-1 related opportunistic infection or other condition requiring acute therapy at the time of randomization.
  • Subjects with acute Hepatitis B and/or C within 30 days of randomization.
  • Previous use of Darunavir or etravirine

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
UK- 453,061 Dose TwoUK-453,061 Dose 2-
ComparatorEtravirine-
UK- 453,061 Dose OneUK-453,061 Dose 1-
Primary Outcome Measures
NameTimeMethod
Percentage of Participants With Human Immunodeficiency Virus Type 1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than (<) 50 Copies/Milliliter (mL) at Week 24Week 24

Plasma HIV-1 RNA level was determined by the Roche Amplicor HIV-1 Monitor standard assay (version 1.5).

Secondary Outcome Measures
NameTimeMethod
Percentage of Participants With HIV-1 RNA Levels <50 Copies/mL at Week 48 and 96Weeks 48, 96

Plasma HIV-1 RNA level was determined by the Roche Amplicor HIV-1 Monitor standard assay (version 1.5).

Percentage of Participants With HIV-1 RNA Levels <400 Copies/mL at Week 24, 48 and 96Week 24, 48, 96

Plasma HIV-1 RNA level was determined by the Roche Amplicor HIV-1 Monitor standard assay (version 1.5).

Change From Baseline in log10 Transformed HIV-1 RNA Levels at Week 24, 48 and 96Baseline, Week 24, 48, 96

Plasma HIV-1 RNA level was determined by the Roche Amplicor HIV-1 Monitor standard assay (version 1.5). For the log10 scale, all the HIV-1 RNA levels were log10 transformed prior to the average calculations. Baseline value calculated as average of measurements collected prior to and including Day 1 pre-dose.

Percentage of Participants With Response as Determined by the Time to Loss of Virologic Response (TLOVR50) Algorithm at Week 24, 48 and 96Week 24, 48, 96

TLOVR50 response (50 denotes lower limit of quantification \[LLOQ\] of assay=50 copies/mL): compliment to TLOVR50 failure. TLOVR50 failure based on observed HIV-1 RNA levels and failure events (death; permanent discontinuation of drug; lost to follow-up; new ARV drug; met treatment failure \[TF\] criteria). TF: an increase of at least (\>=)3 times the baseline plasma HIV-1 RNA level at Week 2 or thereafter; failure to achieve HIV-1 RNA level \<50 copies/mL at Week 24; starting at Week 2, an increase in HIV-1 RNA level to detectable levels (\>50 copies/mL); HIV-1 RNA \<1 log10 decrease from baseline at Week 4 or thereafter. TF were confirmed by second measurement \>=14 days after first. Baseline value was calculated as the average of the measurements collected prior to and including Day 1 pre-dose.

Change From Baseline in Cluster of Differentiation 4 (CD4+) Absolute Lymphocyte Counts at Week 24, 48 and 96Baseline, Week 24, 48, 96

Blood samples for immunological status assessed by CD4+ lymphocyte count. Baseline value was calculated as the average of the measurements collected prior to and including Day 1 pre-dose.

Change From Baseline in Cluster of Differentiation 4 (CD4+) Percentage Lymphocyte Counts at Week 24, 48, 96Baseline, Week 24, 48, 96

Blood samples for immunological status assessed by CD4+ lymphocyte count. Baseline value was calculated as the average of the measurements collected prior to and including Day 1 pre-dose.

Number of Participants With Non-nucleoside Reverse Transcriptase Inhibitors (NNRTI) Resistance-Associated Mutations (RAMs) and/or Phenotypic Susceptibility at Time of Treatment Failure Through Week 48Baseline through Week 48

Genotypic and phenotypic resistance to NNRTIs based on International Acquired Immunodeficiency Syndrome (AIDS) Society, United States of America (IAS-USA) RAM guidelines were evaluated using Monogram Biosciences PhenoSenseGT Assay at Baseline. This was then repeated for all participants with HIV-1 viral load \>500 copies/mL at treatment failure, up to Week 48.

Number of Participants With Laboratory Test AbnormalitiesBaseline up to Week 48 or early termination

Laboratory analysis included blood chemistry, hematology and urinalysis.

Population Pharmacokinetics (PK) of LersivirineWeeks 2, 4, 8, 12, 16, 24, 32, 40, 48

Data for this Outcome Measure are not reported here because the analysis population includes participants who were not enrolled in this study. ClinicalTrials.gov is designed for reporting results from only those participants who were enrolled in the study and described in the Participant Flow and Baseline Characteristics modules.

Lersivirine Success Percentage With Reference to Median Minimum Observed Plasma Concentration (Cmin)Weeks 2, 4, 8, 12, 16, 24, 32, 40, 48

Simple quartile exposure analysis of success rate (viral load \<50 copies/mL) versus median Cmin assesses the exposure response relationship. Percentage of participants with HIV-1 RNA level \<50 copies/mL at median Cmin quartile were planned to be reported.

Time-Averaged Difference (TAD) in log10 Transformed HIV-1 RNA Levels at Week 24, 48 and 96Week 24, 48, 96

TAD was calculated as (area under the curve of HIV-1 RNA levels \[log10 copies/mL\] from baseline to the time point of interest divided by time period in weeks) minus baseline HIV-1 RNA level (log10 copies/mL). Baseline value calculated as average of measurements collected at prior to and including Day 1 pre-dose. Due to early termination of the study decision was made not to derive TAD results for Week 96.

Trial Locations

Locations (63)

Hospital Nossa Senhora da Conceicao

🇧🇷

PoA, RS, Brazil

Hillsborough County Health Department

🇺🇸

Tampa, Florida, United States

Ruth M. Rothstein CORE Center

🇺🇸

Chicago, Illinois, United States

Orlando Immunology Center

🇺🇸

Orlando, Florida, United States

Oddzial do Leczenia HIV

🇵🇱

Szczecin, Poland

Hospital de Joaquim Urbano

🇵🇹

Porto, Portugal

UPR-CTU Pharmacy

🇵🇷

San Juan, Puerto Rico

Rosedale Infectious Diseases

🇺🇸

Huntersville, North Carolina, United States

Klinikum der Universitaet zu Koeln, Klinik I fuer Innere Medizin

🇩🇪

Koeln, Germany

University of California Davis Medical Center

🇺🇸

Sacramento, California, United States

U.O.S. Immunologia Clinica

🇮🇹

Roma, Italy

University Malaya Medical Centre

🇲🇾

Kuala Lumpur, Malaysia

HOPE Clinical Research

🇵🇷

San Juan, Puerto Rico

Lugansk Regional Center of AIDS prophylaxis and control

🇺🇦

Lugansk, Ukraine

AIDS Research Consortium of Atlanta

🇺🇸

Atlanta, Georgia, United States

Nassau University Medical Center

🇺🇸

East Meadow, New York, United States

203 Maxwell Centre

🇿🇦

Durban, Kwazulu-natal, South Africa

Instituto de Infectologia Campinas

🇧🇷

Campinas, SP, Brazil

Hospital Universitario La Paz

🇪🇸

Madrid, Spain

Hospitais da Universidade de Coimbra

🇵🇹

Coimbra, Portugal

Donetsk Regional Center of AIDSs prophylaxis and control

🇺🇦

Donetsk, Ukraine

Royal Free Hospital

🇬🇧

London, United Kingdom

Unita' Operativa Malattie Infettive

🇮🇹

Bologna, Italy

Ararat Research Center

🇵🇷

Ponce, Puerto Rico

North Manchester General Hospital

🇬🇧

Crumpsall, Greater Manchester, United Kingdom

Hospital Heliopolis

🇧🇷

Sao Paulo, SP, Brazil

Hospital Universitari Germans Trias I Pujol

🇪🇸

Badalona, Barcelona, Spain

SPZOZ Wojewodzki Szpital Zakazny

🇵🇱

Warszawa, Poland

Innovative Care PSC

🇵🇷

Bayamon, Puerto Rico

Vinnitsa Regional center for AIDS Prevention and Control

🇺🇦

Berezyna, Vinnitsa District, Vinnitsa Region, Ukraine

Soweto Clinical Trials Centre

🇿🇦

Johannesburg, Gauteng, South Africa

Royal Infirmary GUM Clinic

🇬🇧

Edinburgh, United Kingdom

Department of Infectious Disease, E-Da Hospital

🇨🇳

Kaohsiung County, Taiwan

Dr. J Fourie Medical Centre

🇿🇦

Dundee, Kwazulu-natal, South Africa

Centro Hospitalar de Lisboa Ocidental, EPE.

🇵🇹

Lisboa, Portugal

Centro Hospitalar de Lisboa - Zona Central - Hospital Santo António Capuchos

🇵🇹

Lisboa, Portugal

Hospital São João

🇵🇹

Porto, Portugal

Willowmead Medical Center

🇿🇦

Cape Town, Western CAPE, South Africa

Veterans General Hospital - Taipei

🇨🇳

Taipei, Taiwan

Infectious Diseases Associates of Northwest Florida, PA

🇺🇸

Pensacola, Florida, United States

Jeffrey Goodman Special Care Clinic

🇺🇸

Los Angeles, California, United States

Office of Anthony Mills, MD, Inc.

🇺🇸

Los Angeles, California, United States

San Francisco Veterans Affairs Medical Center

🇺🇸

San Francisco, California, United States

The Kinder Medical Group

🇺🇸

Miami, Florida, United States

Care Resource

🇺🇸

Miami, Florida, United States

University of Cincinnati Medical Center

🇺🇸

Cincinnati, Ohio, United States

Instituto A.Z. de Pesquisa e Ensino

🇧🇷

Curitiba, PR, Brazil

Saint Hope Foundation - Stafford Clinic

🇺🇸

Stafford, Texas, United States

University of Texas Southwestern Medical Center at Dallas

🇺🇸

Dallas, Texas, United States

Hospital Geral de Nova Iguacu

🇧🇷

Nova Iguacu, RJ, Brazil

Centro de Referencia e Treinamento DST/AIDS

🇧🇷

Sao Paulo, SP, Brazil

Hospital Raja Perempuan Zainab II

🇲🇾

Kota Bharu, Kelantan, Malaysia

University of Puerto Rico - Medical Sciences Campus - Puerto Rico Medical Center

🇵🇷

Rio Piedras, Puerto Rico

University of Witwatersrand

🇿🇦

Johannesburg, Gauteng, South Africa

Chris Hani Baragwanath Hospital

🇿🇦

Soweto, Johannesburg, South Africa

Desmond Tutu HIV Foundation

🇿🇦

Cape Town, Western CAPE, South Africa

Brighton and Sussex University Hospitals NHS Trust

🇬🇧

Brighton, EAST Sussex, United Kingdom

Western General Hospital

🇬🇧

Edinburgh, United Kingdom

Saint Hope Foundation - Bellaire Clinic

🇺🇸

Bellaire, Texas, United States

Saint Hope Foundation - Conroe Clinic

🇺🇸

Conroe, Texas, United States

Nicholaos C. Bellos, MD, PA

🇺🇸

Dallas, Texas, United States

CARES

🇺🇸

Sacramento, California, United States

Greiger Clinic

🇺🇸

Mount Vernon, New York, United States

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