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Phase 1 Completed N=20 Treatment

MK-8527 Single-Dose Trial in HIV-1 Infected Participants (MK-8527-004)

Human Immunodeficiency Virus
Source: ClinicalTrials.gov NCT05494736 ↗
Enrolled (actual)
20
Serious AEs
0.0%
Results posted
Mar 2025
Primary outcomePrimary: Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA) — -1.38; -1.40; -0.80 HIV-1 RNA copies/mL

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.

Outcome Measures

OutcomeResultp-value
PRIMARY
Change From Baseline in Plasma HIV-1 Ribonucleic Acid (RNA)
-1.38; -1.40; -0.80
PRIMARY
Number of Participants Experiencing ≥1 Adverse Event (AE)
5; 5; 2
PRIMARY
Number of Participants Discontinuing From Study Due to an AE
0; 0; 0
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)
29.2; 12.6; 5.53
SECONDARY
Area Under the Concentration-Time Curve From Predose to Infinity (AUC0-inf) of MK-8527-TP in PBMCs
47.7; 24.5; 8.87
SECONDARY
Area Under the Concentration-Time Curve From Predose to Last Measurable Concentration (AUC0-last) of MK-8527-TP in PBMCs
40.9; 17.1; 5.88
SECONDARY
Maximum Concentration (Cmax) of MK-8527-TP in PBMCs
0.270; 0.134; 0.0535
SECONDARY
Concentration at 168 Hours Postdose (C168) of MK-8527-TP in PBMCs
0.111; 0.0484; 0.0224
SECONDARY
Time to Maximum Concentration (Tmax) of MK-8527-TP in PBMCs
24.00; 24.03; 23.91
SECONDARY
Apparent Terminal Half-life (t½) of MK-8527-TP in PBMCs
128.24; 172.09; 80.15
SECONDARY
AUC0-inf of MK-8527 in Plasma
0.0512; NA; NA
SECONDARY
AUC0-last of MK-8527 in Plasma
0.0304; NA; NA
SECONDARY
Clast of MK-8527 in Plasma
0.00388; 0.00433; 0.00417
SECONDARY
Cmax of MK-8527 in Plasma
0.0224; 0.00935; 0.00469
SECONDARY
Tmax of MK-8527 in Plasma
0.50; 0.50; 0.50
SECONDARY
Apparent t½ of MK-8527 in Plasma
3.25; NA; NA
SECONDARY
Correlation Between Intracellular C168 of MK-8527-TP in PBMCs and Change From Baseline in Plasma HIV-1 RNA
NA; NA; NA; -0.342

Eligibility Criteria

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
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05494736). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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