MK-8527 + FTC/TDF for Healthy Subjects
Recruiting in Palo Alto (17 mi)
Age: 18 - 65
Sex: Any
Travel: May be covered
Time Reimbursement: Varies
Trial Phase: Phase 1
Recruiting
Sponsor: Merck Sharp & Dohme LLC
No Placebo Group
Trial Summary
What is the purpose of this trial?The goal of this study is to learn what happens to MK-8527 in a healthy person's body over time, called a pharmacokinetic (PK) study. Researchers want to learn if there is a difference in the healthy person's body when MK-8527 is taken as a single dose (Treatment A) or with the medication Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF) (Treatment B).
Will I have to stop taking my current medications?
The trial information does not specify if you need to stop taking your current medications. It's best to discuss this with the trial coordinators.
What makes the drug MK-8527 + FTC/TDF unique compared to other treatments?
The drug MK-8527 combined with FTC/TDF is unique because it involves a novel compound, MK-8527, which is not widely studied or used in standard treatments. This combination may offer a new approach to treatment, potentially with different mechanisms or effects compared to existing therapies.
12345Eligibility Criteria
This clinical trial is open to healthy adults who haven't smoked or used nicotine/tobacco products for at least 3 months and have a BMI between ≥18 and ≤32.0 kg/m2.Participant Groups
The study is examining how MK-8527 behaves in the body over time alone (Treatment A) versus when taken with FTC/TDF (Treatment B), which are medications used in combination therapy.
2Treatment groups
Experimental Treatment
Group I: Treatment B: MK-8527 + FTC/TDFExperimental Treatment2 Interventions
Participants receive FTC/TDF then MK-8527.
Group II: Treatment A: MK-8527Experimental Treatment1 Intervention
Participants receive a single dose of MK-8527.
Find A Clinic Near You
Research locations nearbySelect from list below to view details:
Celerion ( Site 0001)Lincoln, NE
Loading ...
Who is running the clinical trial?
Merck Sharp & Dohme LLCLead Sponsor
References
Further validation to support clinical translation of [(18)F]FTC-146 for imaging sigma-1 receptors. [2022]This study aims to further evaluate the specificity and selectivity of [(18)F]FTC-146 and obtain additional data to support its clinical translation.
Cross-Sectional and Longitudinal Comparison of Tau Imaging with 18F-MK6240 and 18F-Flortaucipir in Populations Matched for Age, MMSE and Brain Beta-Amyloid Burden. [2023]Longitudinal tau quantification may provide a useful marker of drug efficacy in clinical trials. Different tau PET tracers may have different sensitivity to longitudinal changes, but without a head-to-head dataset or a carefully designed case-matching procedure, comparing results in different cohorts can be biased. In this study, we compared the tau PET tracers, 18F-MK6240 and 18F-flortaucipir (FTP), both cross-sectionally and longitudinally by case-matching subjects in the AIBL and ADNI longitudinal cohort studies.
Comparison of New Tau PET-Tracer Candidates With [18F]T808 and [18F]T807. [2018]Early clinical results of two tau tracers, [(18)F]T808 and [(18)F]T807, have recently been reported. In the present study, the biodistribution, radiometabolite quantification, and competition-binding studies were performed in order to acquire comparative preclinical data as well as to establish the value of T808 and T807 as benchmark compounds for assessment of binding affinities of eight new/other tau tracers. Biodistribution studies in mice showed high brain uptake and fast washout.In vivoradiometabolite analysis using high-performance liquid chromatography showed the presence of polar radiometabolites in plasma and brain. No specific binding of [(18)F]T808 was found in transgenic mice expressing mutant human P301L tau. In semiquantitative autoradiography studies on human Alzheimer disease slices, we observed more than 50% tau selective blocking of [(18)F]T808 in the presence of 1 µmol/L of the novel ligands. This study provides a straightforward comparison of the binding affinity and selectivity for tau of the reported radiolabeled tracers BF-158, BF-170, THK5105, lansoprazole, astemizole, and novel tau positron emission tomography ligands against T807 and T808. Therefore, these data are helpful to identify structural requirements for selective interaction with tau and to compare the performance of new highly selective and specific radiolabeled tau tracers.
Impact of spill-in counts from off-target regions on [18F]Flortaucipir PET quantification. [2022]Label="BACKGROUND">[18F]Flortaucipir (FTP) PET quantification is usually hindered by spill-in counts from off-target binding (OFF) regions. The present work aims to provide an in-depth analysis of the impact of OFF in FTP PET quantification, as well as to identify optimal partial volume correction (PVC) strategies to minimize this problem.
Synthesis and Characterization of Fluorine-18-Labeled N-(4-Chloro-3-((fluoromethyl-d2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain. [2021]We have synthesized and characterized [18F]-N-(4-chloro-3-((fluoromethyl-d2)thio)phenyl)-picolinamide ([18F]15) as a potential ligand for the positron emission tomography (PET) imaging of mGluR4 in the brain. Radioligand [18F]15 displays central nervous system drug-like properties, including mGluR4 affinity, potent mGluR4 PAM activity, and selectivity against other mGluRs, as well as sufficient metabolic stability. Radiosynthesis was carried out in two steps. The radiochemical yield of [18F]15 was 11.6 ± 2.9% (n = 7, decay corrected) with a purity of 99% and a molar activity of 84.1 ± 11.8 GBq/μmol. Ex vivo biodistribution studies showed reversible binding of [18F]15 in all investigated tissues including the brain, liver, heart, lungs, and kidneys. PET imaging studies in male Sprague Dawley rats showed that [18F]15 accumulates in the brain regions known to express mGluR4. Pretreatment with the unlabeled mGluR4 PAM compounds 13 (methylthio analogue) and 15 showed significant dose-dependent blocking effects. These results suggest that [18F]15 is a promising radioligand for PET imaging mGluR4 in the brain.