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| ID | Type | Description | Link |
|---|---|---|---|
| MK-8527-004 | Other Identifier | Merck | |
| 2023-503682-39 | Registry Identifier | EU CT | |
| U1111-1287-7295 | Registry Identifier | UTN |
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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Panel A: MK-8527 1.0 mg | Experimental | Participants receive a single oral dose of MK-8527 1.0 mg. |
|
| Panel B: MK-8527 0.5 mg | Experimental | Participants receive a single oral dose of MK-8527 0.5 mg. |
|
| Panel C: MK-8527 0.25 mg | Experimental | Participants receive a single oral dose of MK-8527 0.25 mg. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| MK-8527 | Drug | MK-8527 capsule taken by mouth. |
|
| Measure | Description | Time Frame |
|---|---|---|
| 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. | Baseline and 168 hours postdose on Day 1 |
| 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. | Up to 28 days |
| 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. | Up to 28 days |
| Measure | Description | Time Frame |
|---|---|---|
| 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. | Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose |
| Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs |
Not provided
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 |
|---|---|---|---|---|---|---|
| ARENSIA Exploratory Medicine-Institutul National de Boli Infectioase Matei Bals ( Site 0004) | Bucharest | Bucharest | 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. |
| Label | URL |
|---|---|
| Merck Clinical Trials Information | View source |
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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.
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| ID | Title | Description |
|---|---|---|
| FG000 | Panel A: MK-8527 1.0 mg | Participants receive a single oral dose of MK-8527 1.0 mg on Day 1. |
| FG001 | Panel B: MK-8527 0.5 mg | Participants receive a single oral dose of MK-8527 0.5 mg on Day 1. |
| FG002 | Panel C: MK-8527 0.25 mg | Participants receive a single oral dose of MK-8527 0.25 mg on Day 1. |
| Title | Milestones | Reasons Not Completed | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
There were no participants in Panel D.
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| ID | Title | Description |
|---|---|---|
| BG000 | Panel A: MK-8527 1.0 mg | Participants receive a single oral dose of MK-8527 1.0 mg on Day 1. |
| BG001 | Panel B: MK-8527 0.5 mg | Participants receive a single oral dose of MK-8527 0.5 mg on Day 1. |
| 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 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. | 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. | Posted | Least Squares Mean | 95% Confidence Interval | HIV-1 RNA copies/mL | Baseline and 168 hours postdose on Day 1 |
|
Up to 28 days
All participants who received ≥1 dose of study drug are included.
Not provided
| 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 1.0 mg | Participants receive a single oral dose of MK-8527 1.0 mg on Day 1. |
Not provided
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Conjunctivitis allergic | Eye disorders | MedDRA 27.0 | Systematic Assessment |
Not provided
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Senior Vice President, Global Clinical Development | Merck Sharp & Dohme LLC | 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 | Jul 19, 2023 | Jan 22, 2025 | 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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The MK-8527-TP AUC0-inf in PBMCs is reported. |
| Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
| 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. | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
| Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | The MK-8527-TP Cmax in PBMCs is reported. | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
| Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | The C168 of MK-8527-TP in PBMCs is reported. | 168 hours postdose |
| Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | The MK-8527-TP Tmax in PBMCs is reported. | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
| Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | The apparent t½ of MK-8527-TP in PBMCs is reported. | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
| AUC0-inf of MK-8527 in Plasma | The AUC0-inf of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| AUC0-last of MK-8527 in Plasma | The AUC0-last of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| Clast of MK-8527 in Plasma | The Clast of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| Cmax of MK-8527 in Plasma | The Cmax of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| Tmax of MK-8527 in Plasma | The Tmax of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| Apparent t½ of MK-8527 in Plasma | The apparent t½ of MK-8527 in plasma is reported. | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
| 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. | Predose and 168 hours postdose |
| Josha Research ( Site 0003) |
| Bloemfontein |
| Free State |
| 9301 |
| South Africa |
| Helen Joseph Hospital-Clinical HIV Research Unit ( Site 0002) | Johannesburg | Gauteng | 2092 | South Africa |
| Desmond Tutu Health Foundation ( Site 0001) | Cape Town | Western Cape | 7925 | South Africa |
| Plain Language Summary | View source |
| BG002 | Panel C: MK-8527 0.25 mg | Participants receive a single oral dose of MK-8527 0.25 mg on Day 1. |
| BG003 | 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 |
|
Participants receive a single oral dose of MK-8527 0.5 mg on Day 1.
| OG002 | Panel C: MK-8527 0.25 mg | Participants receive a single oral dose of MK-8527 0.25 mg on Day 1. |
|
|
| 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. | All participants who received ≥1 dose of study therapy are included. | Posted | Count of Participants | Participants | Up to 28 days |
|
|
|
| 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. | All participants who received ≥1 dose of study therapy are included. | Posted | Count of Participants | Participants | Up to 28 days |
|
|
|
| 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. | 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. | Posted | Least Squares Mean | 95% Confidence Interval | h*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, and 168 hours postdose |
|
|
|
| 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. | 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. | Posted | Geometric Mean | 95% Confidence Interval | h*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
|
|
|
| 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. | 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. | Posted | Geometric Mean | 95% Confidence Interval | h*pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
|
|
|
| Secondary | Maximum Concentration (Cmax) of MK-8527-TP in PBMCs | The MK-8527-TP Cmax in PBMCs is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | pmol/10^6 cells | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
|
|
|
| Secondary | Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs | The C168 of MK-8527-TP in PBMCs is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | pmol/10^6 cells | 168 hours postdose |
|
|
|
| Secondary | Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs | The MK-8527-TP Tmax in PBMCs is reported. | 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. | Posted | Median | Full Range | hours | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
|
|
|
| Secondary | Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs | The apparent t½ of MK-8527-TP in PBMCs is reported. | 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. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Predose and 4, 12, 24, 96, 120, 144, 168, 192, 240, 336, 504, and 672 hours postdose |
|
|
|
| Secondary | AUC0-inf of MK-8527 in Plasma | The AUC0-inf of MK-8527 in plasma is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | h*umol/L | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| Secondary | AUC0-last of MK-8527 in Plasma | The AUC0-last of MK-8527 in plasma is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | h*umol/L | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| Secondary | Clast of MK-8527 in Plasma | The Clast of MK-8527 in plasma is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | umol/L | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| Secondary | Cmax of MK-8527 in Plasma | The Cmax of MK-8527 in plasma is reported. | 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. | Posted | Geometric Mean | 95% Confidence Interval | umol/L | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| Secondary | Tmax of MK-8527 in Plasma | The Tmax of MK-8527 in plasma is reported. | 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. | Posted | Median | Full Range | Hours | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| Secondary | Apparent t½ of MK-8527 in Plasma | The apparent t½ of MK-8527 in plasma is reported. | 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. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hours | Predose and 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24 hours postdose |
|
|
|
| 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. | 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. | Posted | Number | Pearson r coefficient | Predose and 168 hours postdose |
|
|
|
| 0 |
| 8 |
| 0 |
| 8 |
| 5 |
| 8 |
| EG001 | Panel B: MK-8527 0.5 mg | Participants receive a single oral dose of MK-8527 0.5 mg on Day 1. | 0 | 6 | 0 | 6 | 5 | 6 |
| EG002 | Panel D: MK-8527 0.25 mg | Participants receive a single oral dose of MK-8527 0.25 mg on Day 1. | 0 | 6 | 0 | 6 | 2 | 6 |
| Diarrhoea | Gastrointestinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Dyspepsia | Gastrointestinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Vessel puncture site bruise | General disorders | MedDRA 27.0 | Systematic Assessment |
|
| Impetigo | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Tinea faciei | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Urinary tract infection | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Carbuncle | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Furuncle | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Hordeolum | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Respiratory syncytial virus infection | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Rhinitis | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Subcutaneous abscess | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Viral rash | Infections and infestations | MedDRA 27.0 | Systematic Assessment |
|
| Contusion | Injury, poisoning and procedural complications | MedDRA 27.0 | Systematic Assessment |
|
| Procedural pain | Injury, poisoning and procedural complications | MedDRA 27.0 | Systematic Assessment |
|
| Skin abrasion | Injury, poisoning and procedural complications | MedDRA 27.0 | Systematic Assessment |
|
| Blood pressure increased | Investigations | MedDRA 27.0 | Systematic Assessment |
|
| Anogenital warts | Neoplasms benign, malignant and unspecified (incl cysts and polyps) | MedDRA 27.0 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 27.0 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 27.0 | Systematic Assessment |
|
| Dyspnoea | Respiratory, thoracic and mediastinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Oropharyngeal pain | Respiratory, thoracic and mediastinal disorders | MedDRA 27.0 | Systematic Assessment |
|
| Dermatitis contact | Skin and subcutaneous tissue disorders | MedDRA 27.0 | Systematic Assessment |
|
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.
| 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 |