The purpose of the study was to assess the steady-state pharmacokinetics (PK) of efavirenz (EFV) in human immunodeficiency virus type 1 (HIV-1) infected subjects on stable antiretroviral regimens containing EFV, and having selected degrees of hepatic impairment or normal hepatic function.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
21
Capsule or Tablet, Oral, once daily for 2 days
Capsule or Tablet, Oral, once daily for 2 days
Capsule or Tablet, Oral, once daily for 2 days
Johns Hopkins University School Of Medicine
Baltimore, Maryland, United States
Uthscsa
San Antonio, Texas, United States
Virginia Commonwealth University Health Systems
Richmond, Virginia, United States
Local Institution
Milan, Italy
Maximum Plasma Concentration (Cmax)
Cmax was obtained directly from the concentration-time data.
Time frame: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.
Minimum Plasma Concentration (Cmin)
Cmin was obtained directly from the concentration-time data.
Time frame: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.
Area Under the Plasma Concentration-time Curve Over the Dosing Interval of 24 Hours (AUC[TAU])
The AUC(TAU), from time 0 to the time of the last measurable concentration (t), was calculated by the linear trapezoidal rule.
Time frame: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Tmax was obtained directly from the concentration-time data.
Time frame: Blood samples were collected at time 0 (pre-dose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12 and 24 hours post-dose, relative to administration of PM or AM dose.
Number of Participants Who Died or Experienced Other Serious Adverse Events (SAEs)
An SAE was defined as any adverse event (AE) occurring at any dose that; resulted in death; was life threatening; resulted in a persistent or significant disability/incapacity; resulted in/prolonged an existing in-patient hospitalization; was a congenital anomaly/birth defect; was a cancer; or was an overdose.
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing). Participants were monitored for SAEs up to 30 days after study discharge.
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Capsule or Tablet, Oral, once daily for 2 days
Number of Participants Who Experienced AEs
AEs were defined as any new untoward medical occurrences or worsening of a pre-existing medical condition in a participant administered a medicinal product, whether or not considered related to the medicinal product.
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing).
Number of Participants Who Experienced AEs Leading to Study Drug Discontinuation
AEs were defined as any new untoward medical occurrences or worsening of a pre-existing medical condition in a participant administered a medicinal product, whether or not considered related to the medicinal product. Participants who discontinued the study due to an AE were recorded.
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing).
Number of Participants With Marked Abnormalities (MAs) in Hematology Measurements
MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following hematology MA definitions specify the criteria for the data presented. Low platelet count: \<0.85 x lower limit of normal (LLN) (or if pre-treatment value \<LLN, then \<0.85 x pre-treatment value). Low leukocytes: \<0.9 x LLN (or if pre-treatment value \<LLN, then \<0.85 x pre-treatment value. If pre-treatment value \>upper limit of normal \[ULN\], then \<LLN). Low neutrophils+bands (absolute): \<=1.500 10\^3 cells/microliter (uL). Low lymphocytes (absolute): \<0.750 10\^3 cells/uL.
Time frame: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.
Number of Participants With Serum Chemistry MAs
MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following serum chemistry MA definitions specify the criteria for MAs in the data presented. High bilirubin (total): \>1.1 x ULN (or if pre-treatment value \>ULN, then \>1.25 x pre-treatment value). High creatinine: \>1.33 x pre-treatment value. Low albumin: \<0.9 x LLN (or if pre-treatment value \<LLN, then \<0.9 x pre-treatment value). High amylase (total): \>2 x pre-treatment value.
Time frame: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.
Number of Participants With Urinalysis MAs
MAs are laboratory measurements marked as abnormal, per pre-defined study criteria, at any study time point. The following urinalysis MA definitions specify the criteria for MAs in the data presented. The presence of white blood cells (WBCs) and red blood cells (RBCs) in the urine was graded on a scale: 0 = no cells present (negative); trace =a small number of cells present; then 1+, 2+, 3+ and 4+, denoting increasingly "positive" urine results (ie, WBCs/RBCs present in the urine). The MA for both WBCs and RBCs was \>= 2+ (or, if pre-treatment value \>=2+, then \>= 4+).
Time frame: Throughout study, from screening (within 21 days of Day 1 dosing) through Day 3.
Number of Participants With Identified Electrocardiogram (ECG) Abnormalities
ECG abnormalities are findings that are clinically meaningful by the judgment of the investigator. A 12-lead ECG was performed and all ECG recordings were evaluated by the investigator. Abnormalities, if present at any study time point, were listed.
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)
Number of Participants With Clinically Meaningful Vital Signs Measures
Vital signs were recorded throughout the study and included investigations related to body temperature, respiratory rate, seated blood pressure (systolic and diastolic), and heart rate. The investigator used his/her clinical judgement to decide whether or not abnormalities in vital signs were clinically meaningful.
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)
Number of Participants With Abnormal Physical Examination Findings at Baseline (Screening and/or Day 1)
The physical examination included an evaluation of the participant's height and body mass index (BMI) (at screening only), and weight. Abnormal physical examination are findings that are clinically meaningful by the judgment of the investigator
Time frame: From screening (within 21 days of Day 1 dosing) to the study discharge day (Day 2 for AM dosing or Day 3 for PM dosing)