Trial Outcomes & Findings for MK-8527 Single-Dose Trial in HIV-1 Infected Participants (MK-8527-004) (NCT NCT05494736)
NCT ID: NCT05494736
Last Updated: 2025-03-26
Results Overview
The mean change from baseline in HIV-1 RNA counts at 168 hours after a single doses of MK-8527 is reported.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
20 participants
Primary outcome timeframe
Baseline and 168 hours postdose on Day 1
Results posted on
2025-03-26
Participant Flow
Participants were recruited at study sites in Romania and South Africa. A total of 4 arms was initially planned, but Arm D was never initiated as the primary objectives were achieved following completion of Arms A to C.
Participant milestones
| Measure |
Panel A: MK-8527 1.0 mg
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
|---|---|---|---|
|
Overall Study
STARTED
|
8
|
6
|
6
|
|
Overall Study
COMPLETED
|
8
|
6
|
6
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
MK-8527 Single-Dose Trial in HIV-1 Infected Participants (MK-8527-004)
Baseline characteristics by cohort
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Total
n=20 Participants
Total of all reporting groups
|
|---|---|---|---|---|
|
Age, Continuous
|
30.0 years
STANDARD_DEVIATION 8.6 • n=5 Participants
|
23.8 years
STANDARD_DEVIATION 3.5 • n=7 Participants
|
37.8 years
STANDARD_DEVIATION 12.6 • n=5 Participants
|
30.5 years
STANDARD_DEVIATION 10.2 • n=4 Participants
|
|
Sex: Female, Male
Female
|
5 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
13 Participants
n=4 Participants
|
|
Sex: Female, Male
Male
|
3 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
7 Participants
n=4 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
8 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
6 Participants
n=5 Participants
|
20 Participants
n=4 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Race (NIH/OMB)
Asian
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Race (NIH/OMB)
Black or African American
|
8 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
16 Participants
n=4 Participants
|
|
Race (NIH/OMB)
White
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
4 Participants
n=4 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
PRIMARY outcome
Timeframe: Baseline and 168 hours postdose on Day 1Population: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The mean change from baseline in HIV-1 RNA counts at 168 hours after a single doses of MK-8527 is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA)
|
-1.38 HIV-1 RNA copies/mL
Interval -1.61 to -1.15
|
-1.40 HIV-1 RNA copies/mL
Interval -1.66 to -1.13
|
-0.80 HIV-1 RNA copies/mL
Interval -1.06 to -0.53
|
—
|
PRIMARY outcome
Timeframe: Up to 28 daysPopulation: All participants who received ≥1 dose of study therapy are included.
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Number of Participants Experiencing ≥1 Adverse Event (AE)
|
5 Participants
|
5 Participants
|
2 Participants
|
—
|
PRIMARY outcome
Timeframe: Up to 28 daysPopulation: All participants who received ≥1 dose of study therapy are included.
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Number of Participants Discontinuing From Study Due to an AE
|
0 Participants
|
0 Participants
|
0 Participants
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The AUC0-168 of MK-8527-TP in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Area Under the Concentration-Time Curve From Predose to 168 Hours Postdose (AUC0-168) of MK-8527 Triphosphate (MK-8527-TP) in Peripheral Blood Mononuclear Cells (PBMCs)
|
29.2 h*pmol/10^6 cells
Interval 24.1 to 35.3
|
12.6 h*pmol/10^6 cells
Interval 10.1 to 15.7
|
5.53 h*pmol/10^6 cells
Interval 4.44 to 6.89
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The MK-8527-TP AUC0-inf in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=5 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs
|
47.7 h*pmol/10^6 cells
Interval 37.8 to 60.3
|
24.5 h*pmol/10^6 cells
Interval 18.7 to 32.1
|
8.87 h*pmol/10^6 cells
Interval 6.6 to 11.9
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The MK-8527-TP AUC0-last in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs
|
40.9 h*pmol/10^6 cells
Interval 32.5 to 51.4
|
17.1 h*pmol/10^6 cells
Interval 13.1 to 22.2
|
5.88 h*pmol/10^6 cells
Interval 4.51 to 7.66
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The MK-8527-TP Cmax in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Maximum Concentration (Cmax) of MK-8527-TP in PBMCs
|
0.270 pmol/10^6 cells
Interval 0.232 to 0.314
|
0.134 pmol/10^6 cells
Interval 0.113 to 0.16
|
0.0535 pmol/10^6 cells
Interval 0.0449 to 0.0637
|
—
|
SECONDARY outcome
Timeframe: 168 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The C168 of MK-8527-TP in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=7 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs
|
0.111 pmol/10^6 cells
Interval 0.0808 to 0.152
|
0.0484 pmol/10^6 cells
Interval 0.0344 to 0.0681
|
0.0224 pmol/10^6 cells
Interval 0.0154 to 0.0325
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The MK-8527-TP Tmax in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs
|
24.00 hours
Interval 12.0 to 24.05
|
24.03 hours
Interval 12.07 to 24.68
|
23.91 hours
Interval 12.0 to 24.12
|
—
|
SECONDARY outcome
Timeframe: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The apparent t½ of MK-8527-TP in PBMCs is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=5 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs
|
128.24 Hours
Geometric Coefficient of Variation 49.00
|
172.09 Hours
Geometric Coefficient of Variation 90.23
|
80.15 Hours
Geometric Coefficient of Variation 52.35
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the lower limit of quantification (LLOQ) are excluded.
The AUC0-inf of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=7 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
AUC0-inf of MK-8527 in Plasma
|
0.0512 h*umol/L
Interval 0.036 to 0.0728
|
NA h*umol/L
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
NA h*umol/L
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
The AUC0-last of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
AUC0-last of MK-8527 in Plasma
|
0.0304 h*umol/L
Interval 0.0221 to 0.0419
|
NA h*umol/L
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
NA h*umol/L
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
The Clast of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=5 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Clast of MK-8527 in Plasma
|
0.00388 umol/L
Interval 0.00346 to 0.00435
|
0.00433 umol/L
Interval 0.0038 to 0.00495
|
0.00417 umol/L
Interval 0.00361 to 0.00482
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
The Cmax of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=5 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Cmax of MK-8527 in Plasma
|
0.0224 umol/L
Interval 0.0172 to 0.0292
|
0.00935 umol/L
Interval 0.00688 to 0.0127
|
0.00469 umol/L
Interval 0.00335 to 0.00656
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
The Tmax of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=5 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Tmax of MK-8527 in Plasma
|
0.50 Hours
Interval 0.5 to 1.0
|
0.50 Hours
Interval 0.5 to 3.0
|
0.50 Hours
Interval 0.23 to 1.0
|
—
|
SECONDARY outcome
Timeframe: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
The apparent t½ of MK-8527 in plasma is reported.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=7 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Apparent t½ of MK-8527 in Plasma
|
3.25 Hours
Geometric Coefficient of Variation 54.52
|
NA Hours
Geometric Coefficient of Variation NA
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
NA Hours
Geometric Coefficient of Variation NA
For all the participants in Panel B and Panel C, only 1 or 2 concentration samples were measurable (in the absorption phase) out of 11 sampling time points collected. All the other concentration data were BLOQ. Therefore, the plasma PK parameters requiring measurable concentrations in the terminal phase were not evaluated for the participants in Panel B and Panel C.
|
—
|
SECONDARY outcome
Timeframe: Predose and 168 hours postdosePopulation: All participants who complied with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model, are included.
The correlation between between the C168 of MK-8527-TP in PBMCs and the change from baseline in plasma HIV-1 RNA levels 168 hours after dosing was calculated based on all pooled participants. All participants who complied with the protocol sufficiently to ensure that generated data will belikely to exhibit the effects of treatment, according to the underlying scientific model, are included. Participants with data below the LLOQ are excluded.
Outcome measures
| Measure |
Panel A: MK-8527 1.0 mg
n=8 Participants
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel C: MK-8527 0.25 mg
n=6 Participants
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
Panels A to C: MK-8527 Pooled
n=20 Participants
All participants who received a single oral dose of MK-8527 are included.
|
|---|---|---|---|---|
|
Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA
|
NA Pearson r coefficient
All arms were pooled to calculate Pearson r.
|
NA Pearson r coefficient
All arms were pooled to calculate Pearson r.
|
NA Pearson r coefficient
All arms were pooled to calculate Pearson r.
|
-0.342 Pearson r coefficient
|
Adverse Events
Panel A: MK-8527 1.0 mg
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Panel B: MK-8527 0.5 mg
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Panel D: MK-8527 0.25 mg
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Panel A: MK-8527 1.0 mg
n=8 participants at risk
Participants receive a single oral dose of MK-8527 1.0 mg on Day 1.
|
Panel B: MK-8527 0.5 mg
n=6 participants at risk
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
|
Panel D: MK-8527 0.25 mg
n=6 participants at risk
Participants receive a single oral dose of MK-8527 0.25 mg on Day 1.
|
|---|---|---|---|
|
Eye disorders
Conjunctivitis allergic
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Gastrointestinal disorders
Diarrhoea
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Gastrointestinal disorders
Dyspepsia
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
General disorders
Vessel puncture site bruise
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Impetigo
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Tinea faciei
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Urinary tract infection
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Carbuncle
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Furuncle
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Hordeolum
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Respiratory syncytial virus infection
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Rhinitis
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Subcutaneous abscess
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Infections and infestations
Viral rash
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Injury, poisoning and procedural complications
Contusion
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Injury, poisoning and procedural complications
Procedural pain
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Injury, poisoning and procedural complications
Skin abrasion
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Investigations
Blood pressure increased
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Neoplasms benign, malignant and unspecified (incl cysts and polyps)
Anogenital warts
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Nervous system disorders
Headache
|
25.0%
2/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Nervous system disorders
Dizziness
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Respiratory, thoracic and mediastinal disorders
Dyspnoea
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Respiratory, thoracic and mediastinal disorders
Epistaxis
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
12.5%
1/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
|
Skin and subcutaneous tissue disorders
Dermatitis contact
|
0.00%
0/8 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
16.7%
1/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
0.00%
0/6 • Up to 28 days
All participants who received ≥1 dose of study drug are included.
|
Additional Information
Senior Vice President, Global Clinical Development
Merck Sharp & Dohme LLC
Phone: 1-800-672-6372
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee If publication activity is not directed by the Sponsor, the investigator agrees to submit all manuscripts or abstracts to the Sponsor before submission. This allows the Sponsor to protect proprietary information and to provide comments.
- Publication restrictions are in place
Restriction type: OTHER