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Phase IIB Pilot of Atazanavir + Raltegravir

Phase 2
Terminated
Conditions
HIV
Interventions
Registration Number
NCT00768989
Lead Sponsor
Bristol-Myers Squibb
Brief Summary

The purpose of this study is to determine if the combination of atazanavir and raltegravir taken together is safe and effective in the treatment of human immunodeficiency virus (HIV).

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
167
Inclusion Criteria
  • Human Immunodeficiency Virus (HIV)-1 positive status

  • HIV ribonucleic acid (RNA) level >=5000 copies/mL

  • Antiretroviral treatment-naive

  • Absolute Cluster of Differentiation 4 (CD4) cell count meeting 1 of the following criteria:

  • <350 cells/mm^3

  • Screening CD4 >=350 and <=500 cells/mm^3 ONLY if at least 1 of the following conditions apply:

    • Screening HIV RNA level >100,000 copies/mL, or
    • CD4 decline >50-100 cells/mm^3/year, or
    • Age >=55 years
  • Any CD4 cell count, if participant has a history of an acquired immune deficiency syndrome-defining illness

  • Medically stable

Exclusion Criteria
  • Screening HIV genotype showing resistance to any component of the study regimen (Atazanavir, Raltegravir, Tenofovir/Emtricitabine)
  • Hepatitis B or hepatitis C coinfection
  • History of or current cardiac disease
  • Electrocardiogram findings:
  • PR Interval >260 msec (severe 1st degree atrioventricular block)
  • QRS Interval >120 msec

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Atazanavir + RaltegravirAtazanavirAtazanavir 300 mg twice daily + Raltegravir 400 mg twice daily
Atazanavir + RaltegravirRaltegravirAtazanavir 300 mg twice daily + Raltegravir 400 mg twice daily
Atazanavir + Ritonavir + Tenofovir /EmtricitabineAtazanavirAtazanavir, 300 mg once daily, + Ritonavir, 100 mg once daily, + Tenofovir 300 mg/Emtricitabine, 200 mg once daily
Atazanavir + Ritonavir + Tenofovir /EmtricitabineRitonavirAtazanavir, 300 mg once daily, + Ritonavir, 100 mg once daily, + Tenofovir 300 mg/Emtricitabine, 200 mg once daily
Atazanavir + Ritonavir + Tenofovir /EmtricitabineTenofovir/EmtricitabineAtazanavir, 300 mg once daily, + Ritonavir, 100 mg once daily, + Tenofovir 300 mg/Emtricitabine, 200 mg once daily
Primary Outcome Measures
NameTimeMethod
Number of Participants With Human Immunodeficiency Virus (HIV) Ribonucleic Acid (RNA) Level <50 Copies/mL at Week 24At Week 24 from Baseline

The number of HIV 1-infected treatment-naive participants with an HIV RNA level \<50 copies/mL after 24 weeks of treatment. Confirmed virologic response noncompleter=failure (NC=F); noncompleter=missing (NC=M); virologic response-observed cases (VR-OC).

Secondary Outcome Measures
NameTimeMethod
Number of Nonresponders at Week 8At Week 8 from Baseline

Participants were classified as nonresponders if they had an HIV RNA level ≥400 copies/mL and a decrease from baseline \<2 log10 copies/mL.

Number of Participants With HIV RNA Levels <50 Copies/mL at Weeks 48 and 96At Weeks 48 and 96 from Baseline

Participant HIV RNA level was determined at Weeks 48 and 96 using the Roche Amplicor® Ultrasensitive Assay Version 1. VR-OC=Virologic response-observed cases.

Number of Participants With HIV RNA Levels <400 Copies/mL at Week 24At Week 24 from Baseline

NC=F: noncompleter=failure; NC=M: noncompleter=missing; VR-OC: virologic response-observed

Number of Participants With HIV RNA Levels <400 Copies/mL at Week 48At Week 48 from Baseline
Number of Participants With HIV RNA Levels <400 Copies/mL at Week 96At Week 96 from Baseline
Mean Change From Baseline in Absolute Cluster of Differentiation 4 Cell CountFrom Baseline to Weeks 2, 4, 8, 12, 16, 20, and 24
Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), Death as Outcome, AEs Leading to Discontinuation, SAEs Leading to DiscontinuationWeek 1 to Week 96, continuously

AE=any new untoward medical occurrence or worsening of a preexisting medical condition that does not necessarily have a causal relationship with this treatment. SAE=any untoward medical occurrence that at any dose results in death, is life-threatening, requires inpatient hospitalization or causes prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, results in drug dependency or drug abuse, or is an important medical event.

Baseline and Mean Change From Baseline in Total Cholesterol LevelsFrom Baseline to Week 24 and Week 48

The mean change from baseline in participant fasting lipids was determined using fasting serum samples.

Mean Change From Baseline in Total Bilirubin LevelFrom Baseline to Week 24 and Week 48
Mean Change From Baseline in Electrocardiogram FindingsFrom Baseline to Week 24

The incidence of QRS wave widening and QT and PR prolongation on participant electrocardiogram findings were evaluated at study Week 24.

Atazanavir Maximum Observed Plasma Concentration (Cmax) in 1 Dosing IntervalAt Week 2 from Baseline

Serial blood samples were collected over a 12-hour period after the morning dose at Week 2.

Raltegravir Cmax in 1 Dosing IntervalAt Week 2 from Baseline

Serial blood samples were collected over a 12-hour period after the morning dose at Week 2.

Atazanavir Time of Maximum Observed Plasma Concentration (Tmax)At Week 2 from Baseline

Serial blood samples were collected over a 12-hour period after the morning dose at Week 2.

Raltegravir TmaxAt Week 2 from Baseline

Serial blood samples were collected over a 12-hour period after the morning dose at Week 2.

Atazanavir Trough Plasma Concentration (Cmin) 12 Hours PostdoseAt Week 2 from Baseline
Raltegravir Cmin 12 Hours PostdoseAt Week 2 from Baseline
Atazanavir Cmin Prior to the Morning DoseAt Week 2 from Baseline
Raltegravir Cmin Prior to the Morning DoseAt Week 2 from Baseline
Atazanavir Area Under the Concentration Curve From Time 0 to 12 Hours (AUC [0-12h]) in 1 Dosing IntervalAt Week 2 from Baseline
Raltegravir AUC (0-12h) in 1 Dosing IntervalAt Week 2 from Baseline
Atazanavir Area Under the Concentration Curve From Time 0 to 24 Hours (AUC [0-24h]) in 1 Dosing IntervalAt Week 2 from Baseline

AUC (0-24h) was estimated by multiplying AUC (0-12h) by 2.

Atazanavir Individual Inhibitory Quotient (IQ)At Week 2 from Baseline

Individual IQ was defined at Cmin at Week 2 divided by the protein binding adjusted EC90 (ie, the drug concentration observed to inhibit virion production by 90% in a cell-based assay) values for Atazanavir that were derived from individual participant clinical isolates.

Atazanavir Terminal Elimination Half LifeAt Week 2 from Baseline
Raltegravir Terminal Elimination Half LifeAt Week 2 from Baseline
Number of Participants With Hematology Laboratory Test Results With Worst Toxicity of Grades 1 to 4 Among All Treated ParticipantsWhile on treatment from Baseline through Week 96

ULN=upper limit of normal. Hematocrit(%) Grade (Gr) 1: ≥28.5-\<31; Gr 2: ≥24-\<28.5; Gr 3: ≥19.5-\<24; Gr 4: \<19.5. Hemoglobin (g/dL) Gr 1: 9.5-11; Gr 2: 8-9.4; Gr 3: 6.5-7.9; Gr 4: \<6.5. Platelets (/mm\^3) Gr 1: 75,000-99,000; Gr 2: 50,000-74,999; Gr 3: 20,000-49,999; Gr 4: \<20,000. White Blood Cells (/mm\^3) Gr 1: \>2500-4000; Gr 2: \>1000-\<2500; Gr 3: \>800-\<1000; Gr 4: \<800. . Prothrombin time (seconds) Gr 1: 1.01-1.25\*ULN; Gr 2: 1.26-1.5\*ULN; Gr 3: 1.51-3\*ULN; Gr 4: \>3\*ULN.

Number of Participants With Blood Chemistry Laboratory Test Results With Worst Toxicity of Grades 1 to 4While on treatment from Baseline through Week 96

Blood urea nitrogen Gr 1:1.25-2.5\*ULN;Gr 2:2.6-5.0\*ULN; Gr 3:5.1-10\*ULN; Gr 4:\>10\*ULN. Creatinine (mg/dL) Gr 1: 1.1-1.5 \*ULN; Gr 2: 1.6-3\*ULN: Gr 3: 3.1-6\*ULN; Gr 4: \>6\*ULN. Hypercarbia (meq/L)Gr 1: 33-36; Gr 2:37-40; Gr 3: 41-45; Gr 4:\>45. Hypocarbia (meq/L)Gr 1:19-21; Gr 2: 15-18; Gr 3: 10-14; Gr 4:\<10. Hypercalcemia (mg/dL)Gr 1:10.6-11.5;Gr 2:11.6-12.5; Gr 3:12.6-13.5;Gr 4: \>13.5. Hypocalcemia (mg/dL)Gr 1: 8.4-7.8;Gr 2:7.7-7; Gr 3:6.9-6.1; Gr 4: \<6.1.Hyperchloremia(meq/L)Gr 1:113-116; Gr 2:117-120; Gr 3:121-125; Gr 4: \>125.Hypochloremia(meq/L)Gr 1: 90-93; Gr 2: 85-89; Gr 3:80-84; Gr 4:\<80.

Number of Participants With Blood Chemistry Laboratory Test Results With Worst Toxicity of Grades 1 to 4 (Continued)While on treatment from Baseline through Week 96

Hyperkalemia(meq/L) Gr 1: 5.6-6; Gr 2: 6.1-6.5; Gr 3: 6.6-7; Gr4: \>7. Hypokalemia(meq/L) Gr 1: 3-3.4; Gr 2: 2.5-2.9; Gr 3: 2-2.4; Gr 4:\<2. Hypernatremia (meq/L) Gr 1: 148-150; Gr 2: 151-157; Gr 3: 148-165; Gr 4: \>165. Hyponatremia (meq/L) Gr 1: 130-132; Gr 2: 123-129; Gr 3: 116-122; Gr 4: \>115.Hyperglycemia(mg/dL)Gr 1: 116-160; Gr 2: 161-250; Gr 3: 251-500; Gr 4: \>500. Hypoglycemia(mg/dL)Gr 1: 55-64; Gr 2: 40-54; Gr 3:30-39;Gr 4:\<30.Creatine kinase (IU/L) Gr 1: \>ULN-1.5\*ULN; Gr 2: 1.5-3\*ULN; Gr 3: \>3-6\*ULN; Gr 4: \>6.0\*ULN. Albumin (g/dL) Gr 1: \<LLN-30; Gr 2: \<30-20; Gr 3\&4: \<20.

Number of Participants With Enzyme and Urine Laboratory Test Results With Worst Toxicity of Grades 1 to 4While on treatment from Baseline through Week 96

AST/SGOT=Aspartate aminotransferase/serum glutamate oxaloacetate transaminase; ALT/SGPT=Alanine transaminase/serum glutamic pyruvic transaminase. Bilirubin (mg/dL)Gr 1: 1.1-1.5\*ULN;Gr 2:1.6-2.5\*ULN;Gr3:2.6-5\*ULN;Gr4:\>5\*ULN.AST/SGOT(U/L)Gr 1:1.25-2.5\*ULN;Gr 2: 2.6-5\*ULN;Gr 3:5.1-10\*ULN;Gr4:\>10\*ULN.ALT/SGPT (U/L)Gr 1:1.25-2.5\*ULN;Gr 2:1.4-2.09\*ULN;Gr 3:5.1-10\*ULN;Gr4:\>10\*ULN. Lipase(U/L)Gr 1:1.1-1.39\*ULN;Gr 2:\>1.5-2\*ULN;Gr 3:2.5-5;Gr 4:5\*ULN.Proteinuria(g/24 hr loss)Gr 1:1+or \<1;Gr 2:2-3+or\>1-2; Gr 3:4+or\>2-3.5;Gr4:\>3.5.Creatine kinase(IU/L)Gr1:2-3\*ULN;Gr 2:3.1-5\*ULN;Gr 3:5.1-10\*ULN;Gr4:\>10\*ULN.

Trial Locations

Locations (10)

Orlando Immunology Center

🇺🇸

Orlando, Florida, United States

Local Institution

🇫🇷

Paris Cedex 20, France

Yale University School Of Medicine

🇺🇸

New Haven, Connecticut, United States

The Aaron Diamond AIDS Research Center

🇺🇸

New York, New York, United States

Southwest Center For HIV/AIDS

🇺🇸

Phoenix, Arizona, United States

Dupont Circle Physicians Group

🇺🇸

Washington, District of Columbia, United States

Therapeutic Concepts, P.A.

🇺🇸

Houston, Texas, United States

Tarrant County Infectious Disease Associates

🇺🇸

Ft Worth, Texas, United States

Diversified Medical Practices, P.A.

🇺🇸

Houston, Texas, United States

University Of Cincinnati

🇺🇸

Cincinnati, Ohio, United States

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