| Primary | Time-Weighted Average Change From Baseline up to Day 11 (DAVG11) in Plasma HIV-1 RNA | DAVG11 was defined as the time-weighted average between the first postbaseline value through the last available on-treatment (ie, the last dose date + 1) value up to Day 11 minus the baseline value in plasma HIV-1 RNA (log10 copies/mL). All HIV-1 RNA data up to Day 11 were used for this analysis. DAVG11 was calculated using the trapezoidal rule and the area-under-the-curve concept. | The Per-Protocol Analysis Set included all randomized participants who took at least 1 dose of bictegravir with baseline HIV-1 RNA ≥ 1900 copies/mL, which allowed up to 2 log decreases in HIV-1 RNA. | Posted | | Mean | Standard Deviation | log10 copies/mL | | Baseline up to Day 11 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days | | OG004 | Placebo | Placebo matched to bictegravir tablet administered orally once daily for 10 days |
| | | Title | Denominators | Categories |
|---|
| Baseline | | | Title | Measurements |
|---|
| - OG0004.26± 0.157
- OG0014.64± 0.498
- OG0024.42± 0.458
- OG003
|
|
| | Group IDs | Group Description | Statistical Method | Statistical Comment | P-Value | P-Value Comment | Parameter Type | Parameter Value | Dispersion Type | Dispersion Value | Confidence Interval Sides | Confidence Interval % | CI Lower Limit | CI Upper Limit | CI Lower Limit Comment | CI Upper Limit Comment | Estimate Comment | Tested Non-Inferiority | Non-Inferiority Type | Non-Inferiority Comment | Other Analysis Description |
|---|
| | t-test, 2 sided | | <0.001 | Comparison was made using the t-test at a 2-sided 0.05 significance level. | | | | | | | | | | | | | Other | | | | | t-test, 2 sided | | <0.001 |
|
| Secondary | Percentage of Participants Who Experienced Treatment-Emergent Adverse Events (AEs) | | The Safety Analysis Set included participants who were randomized and received at least 1 dose of bictegravir or matched placebo. | Posted | | Number | | percentage of participants | | First dose date up to last dose date plus 30 days (Maximum: 40 days) | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days | | OG004 | Placebo | |
|
| Secondary | Percentage of Participants Who Experienced Graded Laboratory Abnormalities | A treatment-emergent graded laboratory abnormality was defined as an increase of at least 1 toxicity grade from predose assessment and occurring after the predose visit and on or before the date of the last dose of study drug plus 30 days. If the predose assessment was missing, then any abnormality of at least Grade 1 associated with the study drug was considered a treatment-emergent graded laboratory abnormality. The most severe graded abnormality from all tests was counted for each participant. | Participants in the Safety Analysis Set were analyzed. | Posted | | Number | | percentage of participants | | First dose date up to last dose date plus 30 days (Maximum: 40 days) | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 |
|
| Secondary | Maximum Reduction From Baseline Through Day 17 in Plasma HIV-1 RNA | Maximum reduction from baseline was defined as the minimum of change from baseline in plasma HIV-1 RNA (i.e. smallest change in HIV-RNA from baseline). | Participants in the Per-Protocol Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | log10 copies/mL | | Baseline to Day 17 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days | | OG004 |
|
| Secondary | Viral Decay Slope in Plasma HIV-1 RNA | Viral Decay Slope = (log10 [HIV-1 RNA on Day x] - log10 [HIV-1 RNA on Day 1]) / (x-1), where x is the collection day of the last available on treatment HIV-1 RNA collected up to Day 7. | Participants in the Per-Protocol Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | log10 copies/mL | | Baseline up to Day 11 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days | | OG004 |
|
| Secondary | Percentage of Participants With HIV-1 RNA < 50 Copies/mL | | Participants in the Per-Protocol Analysis Set were analyzed. | Posted | | Number | | percentage of participants | | Day 17 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days | | OG004 | Placebo | Placebo matched to bictegravir tablet administered orally once daily for 10 days |
|
| Secondary | Pharmacokinetic (PK) Parameter: Cmax of Bictegravir Following Single-Dose and Multiple-Dose Administration | Cmax is defined as the maximum concentration of drug. | The PK Analysis Set included all participants who were randomized and received at least 1 dose of bictegravir and had at least 1 nonmissing concentration of bictegravir. | Posted | | Mean | Standard Deviation | ng/mL | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 for single dose and Day 10 for multiple dose | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
|
| Secondary | PK Parameter: Tmax of Bictegravir Following Single-Dose and Multiple-Dose Administration | Tmax is defined as the time (observed time point) of Cmax. | Participants in the PK Analysis Set were analyzed. | Posted | | Median | Inter-Quartile Range | hours | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 for single dose and Day 10 for multiple dose | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: AUC0-24 of Bictegravir Following Single-Dose Administration | AUC0-24 is defined as the concentration of drug over time from time zero to time 24 hours. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | ng*hr/mL | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: AUClast of Bictegravir Following Single-Dose Administration | AUClast is defined as the concentration of drug from time zero to the last observable concentration. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | ng*hr/mL | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: AUCtau of Bictegravir Following Multiple-Dose Administration | AUCtau is defined as concentration of drug over time (the area under the concentration verses time curve over the dosing interval). | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | ng*hr/mL | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: t1/2 of Bictegravir Following Multiple-Dose Administration | t1/2 is defined as the estimate of the terminal elimination half-life of the drug. | Participants in the PK Analysis Set were analyzed. | Posted | | Median | Inter-Quartile Range | hours | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: Ctau of Bictegravir Following Multiple-Dose Administration | Ctau is defined as the observed drug concentration at the end of the dosing interval. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | ng/mL | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: CLss/F of Bictegravir Following Multiple-Dose Administration | CLss/F is defined as the apparent oral clearance following multiple-dose administration of the drug. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | mL/hr | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: AR_AUC of Bictegravir Following Multiple-Dose Administration | Accumulation ratio of AUC (AR_AUC) = AUCtau on Day 10 / AUC0-24 on Day 1. Percentage of accumulation ratio has been reported. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | percentage of AR_AUC | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 and 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK Parameter: AR_Cmax of Bictegravir Following Multiple-Dose Administration | Accumulation ratio of Cmax (AR_Cmax) = Cmax on Day 10 / Cmax on Day 1. Percentage of accumulation ratio has been reported. | Participants in the PK Analysis Set were analyzed. | Posted | | Mean | Standard Deviation | percentage of AR_Cmax | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 1 and 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days | | OG003 | Bictegravir 100 mg | Bictegravir 100 mg (1 × 100 mg tablet) administered orally once daily for 10 days |
| |
| Secondary | PK/Pharmacodynamic (PD) Analysis: Pearson Correlation Between AUCtau of Bictegravir and DAVG11 in Plasma HIV-1 RNA | AUCtau is defined as concentration of drug over time (the area under the concentration verses time curve over the dosing interval). DAVG11 was defined as the time-weighted average between the first postbaseline value through the last available on-treatment (ie, the last dose date + 1) value up to Day 11 minus the baseline value in plasma HIV-1 RNA (log10 copies/mL). | The PK/PD Analysis Set included all participants in PP Analysis Set (all randomized participants who took at least 1 dose of bictegravir with baseline HIV-1 RNA ≥ 1900 copies/mL, which allowed up to 2 log decreases in HIV-1 RNA) and had both nonmissing bictegravir AUCtau on Day 10 and DAVG11 in log10 plasma HIV-1 RNA. | Posted | | Number | | correlation coefficient | | 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 24 hours postdose at Day 10 | | | | ID | Title | Description |
|---|
| OG000 | Bictegravir 5 mg | Bictegravir 5 mg (1 × 5 mg tablet) administered orally once daily for 10 days | | OG001 | Bictegravir 25 mg | Bictegravir 25 mg (1 × 25 mg tablet) administered orally once daily for 10 days | | OG002 | Bictegravir 50 mg | Bictegravir 50 mg (2 × 25 mg tablets) administered orally once daily for 10 days |
|