An Early Phase 1 interventional study of SULT Allosteric Inhibition in Metabolic Side Effects of Drugs, sponsored by Albert Einstein College of Medicine. Completed at 1 site in United States. Open to male participants aged 61 Years to 61 Years. Per ClinicalTrials.gov, last updated 2023-10-27.
Sponsored by Albert Einstein College of Medicine · Early Phase 1, Interventional, and Basic science
The study test whether the NSAID allosteric site of human sulfotransferase 1A1 (SULT1A1) is operative in humans. The study will test the effects of mefenamic acid (MEF) on the sulfonation of acetaminophen (APAP, a SULT1A1 specific substrate) and dehydroepiandrosterone (DHEA, a SULT2A1 substrate). If the allosteric site is active in vivo, MEF is predicted to result in a decrease in sulfonation of APAP (MEF inhibits SULT with high affinity (Ki = 23 nM), and to have no effect on sulfonation of the DHEA (MEF has little or no effect on SULT2A1 activity).
No patient registries associated with this study.
A single, therapeutic dose of acetaminophen (APAP, 1.0 g)) or dehydroepiandrosterone (DHEA, 75 mg) is taken orally (with 375 ml of water) either alone or simultaneously with a single, oral, therapeutic dose of mefenamic acid (MEF, 0.75 g). In total, 5 experiments will be performed: 1, APAP alone; 2, DHEA alone; 3, MEF alone; 4, APAP + MEF; and 5, DHEA + MEF. Each experiment will be performed in duplicate. Compounds will be taken prior to eating breakfast. One hour later, the patient has a light breakfast (Cheerios and milk, and a cup of coffee) and eats normally thereafter. Urine samples are collected at 15', 30', 1 h, 2h, 3h, 4h, 5 h, 6h, 7h, 8h, 9h, 10h, 11h, and 12h intervals following dosing. The study subject will attempt to completely empty their bladder at each urine-collection time point. The samples are weighed. A 10 ml aliquot is taken from each time point and the aliquots are stored at -20 °C. Samples (0.5 ml) are then transferred to nuclear magnetic resonance (NMR) tubes and NMR spectra are taken to assess drug metabolites in urine. Proton NMR will be performed using the 600 MHz instrument in the Einstein facility.
Albert Einstein College of Medicine is the lead sponsor of 201 studies on the registry; 21 are open to participants now.
Of its 46 completed or terminated interventional studies of FDA-regulated products, 36 (78%) have results posted.
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A single, therapeutic dose of acetaminophen (1.0 g)) or dehydroepiandrosterone (75 mg) is taken orally (with 375 ml of water) either alone or simultaneously with a single, oral, therapeutic dose of mefenamic acid (0.75 g).
Drug: SULT Allosteric Inhibition
A single, therapeutic dose of acetaminophen (APAP, 1.0 g)) or dehydroepiandrosterone (DHEA, 75 mg) is taken orally (with 375 ml of water) either alone or simultaneously with a single, oral, therapeutic dose of mefenamic acid (MEF, 0.75 g). In total, 5 experiments will be performed. Each experiment is performed in duplicate. Compounds are taken prior to eating breakfast. One hour later, the patient has a light breakfast and eats normally thereafter. Urine samples are collected at 15', 30', 1 h, 2h, 3h, 4h, 5 h, 6h, 7h, 8h, 9h, 10h, 11h, and 12h intervals following dosing. The samples are weighed. A 10 ml aliquot is taken from each time point and the aliquots are stored at -20 °C. Samples (0.5 ml) are then transferred to NMR tubes spectra are taken to assess drug metabolites in urine.
Acetaminophen and Dehydroepiandrosterone Conjugates
Proton NMR Signals will be used to quantitate conjugates of acetaminophen and dehydroepiandrosterone in urine.
Time frame: 15min, 30min, 1hr, 2hr, 3hr, 4hr, 5hr, 6hr, 7hr, 8hr, 9hr, 10hr, 11hr, and 12hr following administration.
Plan to share: No — This study will determine the levels acetaminophen and dehydroepiandrosterone conjugates in the urine of a single individuals. The levels will be published and
Ran from Jan 2018 to primary completion in Feb 2023, 60 months.
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This study is completed, as verified in Oct 2023. You cannot join it, but the record below documents what was studied.
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Metabolic Side Effects of Drugs and Substances
Albert Einstein College of Medicine →