Pharmacokinetics and pharmacodynamics of MT-1207, a novel multitarget blocker of α1 receptor, 5-HT2A receptor, and calcium channel, 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-24h 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.