Key result
Single ascending doses of MT-1207 (5-40 mg) were well tolerated in healthy subjects and produced greater blood pressure reductions than placebo between 4 and 24 hours post-administration.
Why the study?
MT-1207 is a novel multitarget blocker under development for hypertension, prompting evaluation of its tolerability, pharmacokinetics, and pharmacodynamics in healthy Chinese subjects.
What are the pharmacokinetics, pharmacodynamics, and tolerability of single ascending doses of MT-1207 in healthy subjects?
RCT (n=56)
What are the pharmacokinetics, pharmacodynamics, and tolerability of single ascending doses of MT-1207 in healthy subjects?
MT-1207, a novel multitarget blocker, is well tolerated and demonstrates dose-dependent antihypertensive effects and predictable pharmacokinetics in healthy subjects.
Background MT-1207 is a novel multitarget blocker of α1 receptor, 5-HT2A receptor, and calcium channel that is currently under development for the treatment of hypertension. In this study, we evaluated the tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of MT-1207 in healthy Chinese subjects.Research design and methods We examined the effects of a single-ascending dose (SAD) of MT-1207 (5–40 mg) and MT-1207 (40 mg) administered in combination with food in 56 healthy subjects.Results No serious adverse events or discontinuations due to adverse events (related to MT-1207) occurred in either study. MT-1207 was rapidly absorbed (median Tmax: 0.5–1.25 h). The mean t1/2 of MT-1207 was approximately 4–7 hours. Systemic exposure (Cmax and AUC) to MT-1207 increased in proportion to dose. Food had little effect on the pharmacokinetics of MT-1207, such as t1/2 and AUC. For 4h–24 h after administration, the blood pressure reduction in the MT-1207 group was higher than that in the placebo group, showing the antihypertensive effect. Blood pressure reduction after MT-1207 administration showed some dose-dependent trend in the 5–20 mg groups.Conclusions MT-1207 was well tolerated in all subjects. PD measurements demonstrated the antihypertensive effects of MT-1207.
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Zhang et al. (2021) conducted an RCT in Healthy subjects (n=56). MT-1207 vs. Placebo was evaluated on Tolerability, pharmacokinetics, and pharmacodynamics. Single ascending doses of MT-1207 (5-40 mg) were well tolerated in healthy subjects and produced greater blood pressure reductions than placebo between 4 and 24 hours post-administration.
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