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| ID | Type | Description | Link |
|---|---|---|---|
| 2018-001861-18 | EudraCT Number | ||
| MK-8527-002 | Other Identifier | Merck Study Number |
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This study will evaluate the anti-retroviral activity of MK-8527 in HIV-1 infected, ART-naïve participants. The primary hypothesis is that MK-8527 has superior anti-retroviral activity compared to placebo, as measured by change from baseline in plasma HIV-1 ribonucleic acid (RNA) at 168 hours postdose.
Up to five panels (Panels A-E) of 6 participants each will be enrolled in a sequential manner. In each panel, participants will receive a single dose of MK-8527 up to 50 mg. Historical data from previous single does studies will be used for placebo (control) comparisons.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Panel A: 10 mg MK-8527 | Experimental | Single oral dose of 10 mg MK-8527 capsule after an 8-hour fast |
|
| Panel B: 3 mg MK-8527 | Experimental | Single oral dose of 3 mg MK-8527 capsule after an 8-hour fast |
|
| Panel C: 1 mg MK-8527 | Experimental | Single oral dose of 1 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
|
| Panel D: ≤50 mg MK-8527 | Experimental | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
|
| Panel E: ≤50 mg MK-8527 | Experimental | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| MK-8527 | Drug | Single oral capsule |
|
| Measure | Description | Time Frame |
|---|---|---|
| Change From Baseline in Plasma HIV-1 RNA | Blood samples were taken to determine HIV-1 RNA levels at Predose (baseline) and 168 hours postdose. Data were fitted with a longitudinal data analysis (LDA) model containing fixed effects for treatment, time and treatment by time interaction, and a random effect for participant.The change from baseline in plasma HIV-1 RNA in participants administered MK-8527 was calculated and results were compared with historical placebo data. | Baseline and 168 hours postdose |
| Percentage of Participants Who Report 1 or More Adverse Events (AEs) | An AE is defined as any untoward medical occurrence in a participant which does not necessarily have a causal relationship with the treatment. An AE is any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it is considered related to the medicinal product. The percentage of participants that reported at least 1 AE will be summarized. | Up to 28 days |
| Percentage of Participants Who Were Discontinued From the Study Due to an AE | An AE is defined as any untoward medical occurrence in a participant which does not necessarily have a causal relationship with the treatment. An AE is any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it is considered related to the medicinal product. The percentage of participants that were discontinued from the study due to an AE will be summarized. | Up to 28 days |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration Time Curve From Hour 0 to 168 Hours (AUC0-168) of MK-8527-TP in Peripheral Blood Mononuclear Cells (PBMC) | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-168 of MK-8527-triphosphate (MK-8527-TP) in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% confidence intervals (CI) for the means were constructed on the natural log scale and referenced the t-distribution. |
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Inclusion Criteria
Exclusion Criteria
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| Name | Affiliation | Role |
|---|---|---|
| Medical Director | Merck Sharp & Dohme LLC | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Matei Bals Infectious Diseases Institute ( Site 0001) | Bucharest | 021105 | Romania |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 41830320 | Derived | Carstens RP, Kapoor Y, Vargo RC, Bhattacharyya A, Garrett G, Cilissen C, Adedoyin A, Zang X, Denef JF, Leyssens C, Reynders T, Preotescu L, Kaplan R, Rassool M, Lombaard J, Streinu-Cercel A, Matthews RP, Stoch SA, Iwamoto M, Gillespie GL. Antiretroviral Activity, Pharmacokinetics, and Safety of MK-8527, an Oral Nucleoside Reverse Transcriptase Translocation Inhibitor, in Adults With HIV-1 Who Had Not Previously Taken Antiretroviral Agents: Results From 2 Open-Label, Phase 1 Studies. Clin Infect Dis. 2026 May 20;82(5):e984-e991. doi: 10.1093/cid/ciag135. |
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Anti-retroviral therapy (ART)-naïve, participants with human immunodeficiency type 1 virus (HIV-1) infection were enrolled in this study.
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| ID | Title | Description |
|---|---|---|
| FG000 | Panel A: MK-8527 10 mg | Single oral dose of 10 mg MK-8527 in capsule form after an 8-hour fast |
| FG001 | Panel B: MK-8527 3 mg | Single oral dose of 3 mg MK-8527 in capsule form after an 8-hour fast |
| FG002 | Panel C: MK-8527 1 mg | Single oral dose of 1 mg MK-8527 in capsule form after an 8-hour fast |
| FG003 | Panel D: ≤50 mg MK-8527 | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
| FG004 | Panel E: ≤50 mg MK-8527 | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
Panels D and E were not conducted as the scientific study objectives were met in the conducted panels.
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| ID | Title | Description |
|---|---|---|
| BG000 | Panel A: MK-8527 10 mg | Single oral dose of 10 mg MK-8527 in capsule form after an 8-hour fast |
| BG001 | Panel B: MK-8527 3 mg | Single oral dose of 3 mg MK-8527 in capsule form after an 8-hour fast |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Change From Baseline in Plasma HIV-1 RNA | Blood samples were taken to determine HIV-1 RNA levels at Predose (baseline) and 168 hours postdose. Data were fitted with a longitudinal data analysis (LDA) model containing fixed effects for treatment, time and treatment by time interaction, and a random effect for participant.The change from baseline in plasma HIV-1 RNA in participants administered MK-8527 was calculated and results were compared with historical placebo data. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Least Squares Mean | 95% Confidence Interval | log10 copies/mL | Baseline and 168 hours postdose |
|
Up to 28 days
Participants who received at least one dose of the investigational drug. Panels D and E were not conducted as the scientific study objectives were met in the conducted panels.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Panel A: MK-8527 10 mg | Single oral dose of 10 mg MK-8527 in capsule form after an 8-hour fast |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Pharyngitis | Infections and infestations | MedDRA 22.1 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Senior Vice President, Global Clinical Development | Merck Sharp & Dohme Corp. | 1-800-672-6372 | ClinicalTrialsDisclosure@merck.com |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot_SAP | Yes | Yes | No | Study Protocol and Statistical Analysis Plan | Jun 7, 2018 | Sep 4, 2020 | Prot_SAP_000.pdf |
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| ID | Term |
|---|---|
| D000163 | Acquired Immunodeficiency Syndrome |
| ID | Term |
|---|---|
| D015658 | HIV Infections |
| D000086982 | Blood-Borne Infections |
| D003141 | Communicable Diseases |
| D007239 | Infections |
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| Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose |
| Area Under the Concentration Time Curve From Hour 0 to Last (AUC0-last) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the AUC0-last of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
| Area Under the Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the AUC0-Inf of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
| Maximum Concentration (Cmax) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the Cmax of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
| Time to Cmax (Tmax) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the Tmax of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
| Concentration at 168 Hours (C168) of MK-8527-TP in PBMC | Blood samples were taken at 168 hours postdose to determine the C168 of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | 168 hours postdose for each panel |
| Apparent Terminal Half Life (t1/2) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the t1/2 of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
| Area Under the Concentration Time Curve From Hour 0 to 168 Hours (AUC0-168) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-168 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| Area Under the Concentration Time Curve From Hour 0 to Last (AUC0-last) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-last of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| Area Under the Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-inf of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| Maximum Concentration (Cmax) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the Cmax of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| Time to Cmax (Tmax) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the Tmax of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| Concentration at 168 Hours (C168) of MK-8527 in Plasma | Blood samples were taken at 168 hours postdose to determine the C168 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | 168 hours postdose |
| Apparent Terminal Half Life (t1/2) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the t1/2 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
| BG002 | Panel C: MK-8527 1 mg | Single oral dose of 1 mg MK-8527 in capsule form after an 8-hour fast |
| BG003 | Panel D: ≤50 mg MK-8527 | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
| BG004 | Panel E: ≤50 mg MK-8527 | Single oral dose of ≤50 mg MK-8527 capsule after an 8-hour fast. Dose level determined by results of previous panels. |
| BG005 | Total | Total of all reporting groups |
| Years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
| Ethnicity (NIH/OMB) | Count of Participants | Participants |
|
| Race (NIH/OMB) | Count of Participants | Participants |
|
Single oral dose of 10 mg MK-8527 in capsule form after an 8-hour fast
| OG001 | Panel B: MK-8527 3 mg | Single oral dose of 3 mg MK-8527 in capsule form after an 8-hour fast |
| OG002 | Panel C: MK-8527 1 mg | Single oral dose of 1 mg MK-8527 in capsule form after an 8-hour fast |
|
|
|
| Primary | Percentage of Participants Who Report 1 or More Adverse Events (AEs) | An AE is defined as any untoward medical occurrence in a participant which does not necessarily have a causal relationship with the treatment. An AE is any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it is considered related to the medicinal product. The percentage of participants that reported at least 1 AE will be summarized. | Participants who received at least one dose of the investigational drug. | Posted | Number | Percentage of participants | Up to 28 days |
|
|
|
| Primary | Percentage of Participants Who Were Discontinued From the Study Due to an AE | An AE is defined as any untoward medical occurrence in a participant which does not necessarily have a causal relationship with the treatment. An AE is any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with use of a medicinal product, regardless of whether or not it is considered related to the medicinal product. The percentage of participants that were discontinued from the study due to an AE will be summarized. | Participants who received at least one dose of the investigational drug. | Posted | Number | Percentage of participants | Up to 28 days |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to 168 Hours (AUC0-168) of MK-8527-TP in Peripheral Blood Mononuclear Cells (PBMC) | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-168 of MK-8527-triphosphate (MK-8527-TP) in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% confidence intervals (CI) for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to Last (AUC0-last) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the AUC0-last of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the AUC0-Inf of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
|
|
|
| Secondary | Maximum Concentration (Cmax) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the Cmax of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
|
|
|
| Secondary | Time to Cmax (Tmax) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the Tmax of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Median | Full Range | Hours | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
|
|
|
| Secondary | Concentration at 168 Hours (C168) of MK-8527-TP in PBMC | Blood samples were taken at 168 hours postdose to determine the C168 of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | pmol/10^6 cells | 168 hours postdose for each panel |
|
|
|
| Secondary | Apparent Terminal Half Life (t1/2) of MK-8527-TP in PBMC | Blood samples were taken at Predose, up to approximately 28 days postdose to determine the t1/2 of MK-8527-TP in PBMCs. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Predose and 4, 12, 24, 96, 120, 144, 168, 240, 336, 504, 672 hours or 28 days postdose |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to 168 Hours (AUC0-168) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-168 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. The 1 mg MK-8527 arm had insufficient data for one participant. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*μmol/L | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to Last (AUC0-last) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-last of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*μmol/L | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| Secondary | Area Under the Concentration Time Curve From Hour 0 to Infinity (AUC0-inf) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the AUC0-inf of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. The 1 mg MK-8527 arm had insufficient data for four participants. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | hr*μmol/L | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| Secondary | Maximum Concentration (Cmax) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the Cmax of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | μmol/L | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| Secondary | Time to Cmax (Tmax) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the Tmax of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Median | Full Range | Hours | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| Secondary | Concentration at 168 Hours (C168) of MK-8527 in Plasma | Blood samples were taken at 168 hours postdose to determine the C168 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | 95% Confidence Interval | μmol/L | 168 hours postdose |
|
|
|
| Secondary | Apparent Terminal Half Life (t1/2) of MK-8527 in Plasma | Blood samples were taken at Predose, up to 168 hours postdose to determine the t1/2 of MK-8527 in plasma. Values were natural log transformed and analyzed based on a linear model containing a fixed effect for dose level. The 95% CI for the means were constructed on the natural log scale and referenced the t-distribution. | Participants who comply with the protocol sufficiently to ensure that generated data will be likely to exhibit the effects of treatment, according to the underlying scientific model. The 1 mg MK-8527 arm had insufficient data for four participants. Participants from Panels D and E were not analyzed because they were not enrolled in the study. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Predose and 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, and 168 hours postdose |
|
|
|
| 0 |
| 6 |
| 0 |
| 6 |
| 0 |
| 6 |
| EG001 | Panel B: MK-8527 3 mg | Single oral dose of 3 mg MK-8527 in capsule form after an 8-hour fast | 0 | 6 | 0 | 6 | 2 | 6 |
| EG002 | Panel C: MK-8527 1 mg | Single oral dose of 1 mg MK-8527 in capsule form after an 8-hour fast | 0 | 5 | 0 | 5 | 0 | 5 |
| Dizziness | Nervous system disorders | MedDRA 22.1 | Systematic Assessment |
|
| Insomnia | Psychiatric disorders | MedDRA 22.1 | Systematic Assessment |
|
Not provided
Not provided
| D015229 |
| Sexually Transmitted Diseases, Viral |
| D012749 | Sexually Transmitted Diseases |
| D016180 | Lentivirus Infections |
| D012192 | Retroviridae Infections |
| D012327 | RNA Virus Infections |
| D014777 | Virus Diseases |
| D012897 | Slow Virus Diseases |
| D000091662 | Genital Diseases |
| D000091642 | Urogenital Diseases |
| D007153 | Immunologic Deficiency Syndromes |
| D007154 | Immune System Diseases |