Human Immunodeficiency Virus
Conditions
Brief summary
This is a single-dose clinical study to evaluate the safety, tolerability, pharmacokinetics, and anti-retroviral activity of MK-8527 in antiretroviral therapy (ART)-naïve participants living with human immunodeficiency virus type 1 (HIV-1) infection. The primary hypothesis is that, at a dose that is safe and generally well tolerated, MK-8527 will have antiretroviral activity as measured by a reduction from baseline in plasma HIV-1 ribonucleic acid (RNA) of ≥1.0 log10 copies/mL. 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.
Interventions
DRUGMK-8527
MK-8527 capsule taken by mouth.
Sponsors
Merck Sharp & Dohme LLC
Study design
Allocation
NON_RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 60 Years
Healthy volunteers
No
Inclusion criteria
* Is in good health other than HIV-1 infection * Is documented HIV-1 positive * Is ART-naïve, which is defined as not having received any marketed antiretroviral agent for treatment of HIV-1 infection (prior use of an ART for PrEP or investigational therapy is permitted if the last dose was ≥30 days prior to study drug administration) * Is willing to receive no other ART for the monitoring period of this study
Exclusion criteria
* Has a history of clinically significant endocrine, GI, cardiovascular, hematological, hepatic, immunological (outside of HIV-1 infection), renal, respiratory, genitourinary, or major neurological (including stroke and chronic seizures) abnormalities or diseases * Is unable to refrain from or anticipates the use of any medication, including prescription and nonprescription drugs or herbal remedies beginning approximately 2 weeks (or 5 half-lives) prior to administration of the initial dose of study intervention, throughout the study, until the poststudy visit * Has participated in another investigational study within 4 weeks (or 5 half-lives, whichever is greater) prior to the prestudy (screening) visit
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA) | Baseline and 168 hours postdose on Day 1 | The mean change from baseline in HIV-1 RNA counts at 168 hours after a single doses of MK-8527 is reported. |
| Number of Participants Experiencing ≥1 Adverse Event (AE) | Up to 28 days | 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. |
| Number of Participants Discontinuing From Study Due to an AE | Up to 28 days | 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. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose | The MK-8527-TP Cmax in PBMCs is reported. |
| Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | 168 hours postdose | The C168 of MK-8527-TP in PBMCs is reported. |
| Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose | The MK-8527-TP Tmax in PBMCs is reported. |
| Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose | The apparent t½ of MK-8527-TP in PBMCs is reported. |
| AUC0-inf of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The AUC0-inf of MK-8527 in plasma is reported. |
| 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) | Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose | The AUC0-168 of MK-8527-TP in PBMCs is reported. |
| Clast of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The Clast of MK-8527 in plasma is reported. |
| Cmax of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The Cmax of MK-8527 in plasma is reported. |
| Tmax of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The Tmax of MK-8527 in plasma is reported. |
| Apparent t½ of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The apparent t½ of MK-8527 in plasma is reported. |
| Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA | Predose and 168 hours postdose | 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. |
| AUC0-last of MK-8527 in Plasma | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose | The AUC0-last of MK-8527 in plasma is reported. |
| Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose | The MK-8527-TP AUC0-inf in PBMCs is reported. |
| Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose | The MK-8527-TP AUC0-last in PBMCs is reported. |
Countries
Romania, South Africa
Participant flow
Pre-assignment details
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.
Participants by arm
| Arm | Count |
|---|---|
| Panel A: MK-8527 1.0 mg Participants receive a single oral dose of MK-8527 1.0 mg on Day 1. | 8 |
| Panel B: MK-8527 0.5 mg Participants receive a single oral dose of MK-8527 0.5 mg on Day 1. | 6 |
| Panel C: MK-8527 0.25 mg Participants receive a single oral dose of MK-8527 0.25 mg on Day 1. | 6 |
| Total | 20 |
Baseline characteristics
| Characteristic | Panel A: MK-8527 1.0 mg | Panel B: MK-8527 0.5 mg | Panel C: MK-8527 0.25 mg | Total |
|---|---|---|---|---|
| Age, Continuous | 30.0 years STANDARD_DEVIATION 8.6 | 23.8 years STANDARD_DEVIATION 3.5 | 37.8 years STANDARD_DEVIATION 12.6 | 30.5 years STANDARD_DEVIATION 10.2 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 8 Participants | 6 Participants | 6 Participants | 20 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Black or African American | 8 Participants | 6 Participants | 2 Participants | 16 Participants |
| Race (NIH/OMB) More than one race | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 0 Participants | 0 Participants | 4 Participants | 4 Participants |
| Sex: Female, Male Female | 5 Participants | 6 Participants | 2 Participants | 13 Participants |
| Sex: Female, Male Male | 3 Participants | 0 Participants | 4 Participants | 7 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk |
|---|---|---|---|
| deaths Total, all-cause mortality | 0 / 8 | 0 / 6 | 0 / 6 |
| other Total, other adverse events | 5 / 8 | 5 / 6 | 2 / 6 |
| serious Total, serious adverse events | 0 / 8 | 0 / 6 | 0 / 6 |
Outcome results
Primary
Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA)
The mean change from baseline in HIV-1 RNA counts at 168 hours after a single doses of MK-8527 is reported.
Time frame: Baseline and 168 hours postdose on Day 1
Population: 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.
| Arm | Measure | Value (LEAST_SQUARES_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA) | -1.38 HIV-1 RNA copies/mL |
| Panel B: MK-8527 0.5 mg | Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA) | -1.40 HIV-1 RNA copies/mL |
| Panel C: MK-8527 0.25 mg | Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA) | -0.80 HIV-1 RNA copies/mL |
Primary
Number of Participants Discontinuing From Study Due to an AE
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.
Time frame: Up to 28 days
Population: All participants who received ≥1 dose of study therapy are included.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Number of Participants Discontinuing From Study Due to an AE | 0 Participants |
| Panel B: MK-8527 0.5 mg | Number of Participants Discontinuing From Study Due to an AE | 0 Participants |
| Panel C: MK-8527 0.25 mg | Number of Participants Discontinuing From Study Due to an AE | 0 Participants |
Primary
Number of Participants Experiencing ≥1 Adverse Event (AE)
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.
Time frame: Up to 28 days
Population: All participants who received ≥1 dose of study therapy are included.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Number of Participants Experiencing ≥1 Adverse Event (AE) | 5 Participants |
| Panel B: MK-8527 0.5 mg | Number of Participants Experiencing ≥1 Adverse Event (AE) | 5 Participants |
| Panel C: MK-8527 0.25 mg | Number of Participants Experiencing ≥1 Adverse Event (AE) | 2 Participants |
Secondary
Apparent t½ of MK-8527 in Plasma
The apparent t½ of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-8527 1.0 mg | Apparent t½ of MK-8527 in Plasma | 3.25 Hours | Geometric Coefficient of Variation 54.52 |
| Panel B: MK-8527 0.5 mg | Apparent t½ of MK-8527 in Plasma | NA Hours | — |
| Panel C: MK-8527 0.25 mg | Apparent t½ of MK-8527 in Plasma | NA Hours | — |
Secondary
Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs
The apparent t½ of MK-8527-TP in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-8527 1.0 mg | Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | 128.24 Hours | Geometric Coefficient of Variation 49 |
| Panel B: MK-8527 0.5 mg | Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | 172.09 Hours | Geometric Coefficient of Variation 90.23 |
| Panel C: MK-8527 0.25 mg | Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | 80.15 Hours | Geometric Coefficient of Variation 52.35 |
Secondary
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)
The AUC0-168 of MK-8527-TP in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose
Population: 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.
| Arm | Measure | Value (LEAST_SQUARES_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | 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 |
| Panel B: MK-8527 0.5 mg | 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) | 12.6 h*pmol/10^6 cells |
| Panel C: MK-8527 0.25 mg | 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) | 5.53 h*pmol/10^6 cells |
Secondary
Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs
The MK-8527-TP AUC0-inf in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | 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 |
| Panel B: MK-8527 0.5 mg | Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs | 24.5 h*pmol/10^6 cells |
| Panel C: MK-8527 0.25 mg | Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs | 8.87 h*pmol/10^6 cells |
Secondary
Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs
The MK-8527-TP AUC0-last in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | 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 |
| Panel B: MK-8527 0.5 mg | Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs | 17.1 h*pmol/10^6 cells |
| Panel C: MK-8527 0.25 mg | Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs | 5.88 h*pmol/10^6 cells |
Secondary
AUC0-inf of MK-8527 in Plasma
The AUC0-inf of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | AUC0-inf of MK-8527 in Plasma | 0.0512 h*umol/L |
| Panel B: MK-8527 0.5 mg | AUC0-inf of MK-8527 in Plasma | NA h*umol/L |
| Panel C: MK-8527 0.25 mg | AUC0-inf of MK-8527 in Plasma | NA h*umol/L |
Secondary
AUC0-last of MK-8527 in Plasma
The AUC0-last of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | AUC0-last of MK-8527 in Plasma | 0.0304 h*umol/L |
| Panel B: MK-8527 0.5 mg | AUC0-last of MK-8527 in Plasma | NA h*umol/L |
| Panel C: MK-8527 0.25 mg | AUC0-last of MK-8527 in Plasma | NA h*umol/L |
Secondary
Clast of MK-8527 in Plasma
The Clast of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Clast of MK-8527 in Plasma | 0.00388 umol/L |
| Panel B: MK-8527 0.5 mg | Clast of MK-8527 in Plasma | 0.00433 umol/L |
| Panel C: MK-8527 0.25 mg | Clast of MK-8527 in Plasma | 0.00417 umol/L |
Secondary
Cmax of MK-8527 in Plasma
The Cmax of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Cmax of MK-8527 in Plasma | 0.0224 umol/L |
| Panel B: MK-8527 0.5 mg | Cmax of MK-8527 in Plasma | 0.00935 umol/L |
| Panel C: MK-8527 0.25 mg | Cmax of MK-8527 in Plasma | 0.00469 umol/L |
Secondary
Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs
The C168 of MK-8527-TP in PBMCs is reported.
Time frame: 168 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | 0.111 pmol/10^6 cells |
| Panel B: MK-8527 0.5 mg | Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | 0.0484 pmol/10^6 cells |
| Panel C: MK-8527 0.25 mg | Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | 0.0224 pmol/10^6 cells |
Secondary
Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA
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.
Time frame: Predose and 168 hours postdose
Population: 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.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA | NA Pearson r coefficient |
| Panel B: MK-8527 0.5 mg | Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA | NA Pearson r coefficient |
| Panel C: MK-8527 0.25 mg | Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA | NA Pearson r coefficient |
| Panels A to C: MK-8527 Pooled | Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA | -0.342 Pearson r coefficient |
Secondary
Maximum Concentration (Cmax) of MK-8527-TP in PBMCs
The MK-8527-TP Cmax in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose
Population: 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.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | 0.270 pmol/10^6 cells |
| Panel B: MK-8527 0.5 mg | Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | 0.134 pmol/10^6 cells |
| Panel C: MK-8527 0.25 mg | Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | 0.0535 pmol/10^6 cells |
Secondary
Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs
The MK-8527-TP Tmax in PBMCs is reported.
Time frame: Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose
Population: 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.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | 24.00 hours |
| Panel B: MK-8527 0.5 mg | Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | 24.03 hours |
| Panel C: MK-8527 0.25 mg | Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | 23.91 hours |
Secondary
Tmax of MK-8527 in Plasma
The Tmax of MK-8527 in plasma is reported.
Time frame: Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose
Population: 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.
| Arm | Measure | Value (MEDIAN) |
|---|---|---|
| Panel A: MK-8527 1.0 mg | Tmax of MK-8527 in Plasma | 0.50 Hours |
| Panel B: MK-8527 0.5 mg | Tmax of MK-8527 in Plasma | 0.50 Hours |
| Panel C: MK-8527 0.25 mg | Tmax of MK-8527 in Plasma | 0.50 Hours |