This open-label study will evaluate the effect of food on the bioavailability of a single dose of 4-MUST, tablets, 128 mg. Additionally, the study will assess the pharmacokinetics, safety, and tolerability of 4-MUST, tablets, 128 mg following both single and multiple oral dose administration.
Voluntary, personally signed ICF obtained prior to any study procedures;
Males and females aged 18 to 45 years (inclusive) of Caucasian race;
Confirmed healthy status based on the absence of clinically significant abnormalities in clinical, laboratory, and diagnostic assessments specified in the protocol;
Blood pressure (BP): systolic blood pressure (SBP) from 99 to 129 mmHg (inclusive), diastolic blood pressure (DBP) from 70 to 89 mmHg (inclusive);
Voluntary withdrawal of the subject from the study;
Failure to comply with protocol requirements by the volunteer (e.g., missing scheduled study procedures, unauthorized use of prohibited medications, or violation of dietary or lifestyle restrictions);
Occurrence of any event or condition during the study that, in the investigator's judgement, may compromise the volunteer's safety (e.g., hypersensitivity reactions);
Volunteers selected for participation in the study in violation of the inclusion/non-inclusion criteria;
Sequential
4-MUST
Drug128 mg tablets containing trimebutine 4-methylumbelliferyl sulfate (4-MUST)
Pharmacokinetics - Cmax
Maximum plasma concentration (Cmax) of 4-MUST metabolites: trimebutine, N-desmethyltrimebutine, 3,4,5-trimethoxybenzoic acid, 4-methylumbelliferone sulfate, 4-methylumbelliferone and 4-methylumbelliferone glucuronide
Pharmacokinetics - tmax
Time to reach Cmax (tmax) of trimebutine, N-desmethyltrimebutine, 3,4,5-trimethoxybenzoic acid, 4-methylumbelliferone sulfate, 4-methylumbelliferone and 4-methylumbelliferone glucuronide
Pharmacokinetics - AUC0-t
Area under the plasma concentration-time curve from time 0 to t (AUC0-t) of trimebutine, N-desmethyltrimebutine, 3,4,5-trimethoxybenzoic acid, 4-methylumbelliferone sulfate, 4-methylumbelliferone and 4-methylumbelliferone glucuronide
Pharmacokinetics - AUC0-inf
Area under the plasma concentration-time curve from time 0 to infinity (AUC0-inf) of trimebutine, N-desmethyltrimebutine, 3,4,5-trimethoxybenzoic acid, 4-methylumbelliferone sulfate, 4-methylumbelliferone and 4-methylumbelliferone glucuronide
Adverse event type
Adverse events will be assessed by complaints, results of physical examination, results of heart rate and blood pressure assessment, results of respiratory rate assessment, body temperature, laboratory monitoring (clinical blood count, biochemical blood count, urinalysis), electrocardiography; adverse events will be classified in accordance to MedDRA.
Adverse event frequency
Number and frequency of adverse events registered during the study
Adverse event severety
Severity of adverse events registered during the study, assessed using the Common Terminology Criteria for Adverse Events (CTCAE)
Drop-outs associated with adverse events
The number of cases of early termination of participation in the study due to the development of adverse events and/or serious adverse events associated with the study drug
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