This is a randomized, double-blind, placebo-controlled, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of a single dose of MT2004 following oral single and multiple ascending dose administration.
A total of 48 subjects will be evaluated with 36 subjects randomized to receive active drug and 12 subjects randomized to receive placebo in a double-blind fashion (eight subjects per each dose cohort, six subjects randomized to active drug and two subjects randomized to placebo). A separate open panel of 8 subjects will receive a single dose of MT2004 under fed conditions following the last of the SAD dose escalation cohorts. The dose level will be selected by the sponsor based upon the safety and PK data generated in each dose escalation cohort of the SAD part of the trial. A total of 24 subjects will receive MT2004 (8 subjects in each dose cohort for a total of 3 cohorts, 6 subjects randomized to active drug and 2 subjects randomized to placebo per cohort). MT2004 dosing regimens (dose levels and duration of administration) will be determined based on the collective SAD PK and safety data from Part 1 and nonclinical data of MT2004 (pharmacology and toxicology). Tentative dosing regimen is once daily for a consecutive 14 days.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
88
Pharmaron CPC, Inc.
Baltimore, Maryland, United States
Cmax of MT2004
Maximum observed concentration (Cmax) of MT2004
Time frame: 48 hours
AUClast of MT2004
Area under the concentration-time curve (AUC) from Hour 0 to the last measurable concentration (AUC0-last) of MT2004
Time frame: 48 hours
Tmax of MT2004
Time to maximum concentration (Tmax)
Time frame: 48 hours
T half of MT2004
T half of MT2004
Time frame: 48 hours
Plasma FGF19 Level
Plasma FGF19 Level
Time frame: 24 hours
Serum 7-alpha-hydroxy-4-cholesten-3-one (C4) Level
Serum 7-alpha-hydroxy-4-cholesten-3-one (C4) Level
Time frame: 24 hours
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