Phase I study of OPC-8212: 3,4-dihydro-6-(4-(3,4-dimethoxybenzoyl)-1-piperazinyl)-2(1H)-quinolinone, a new oral inotropic agent.

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A phase I study of OPC-8212: 3, 4-dihydro-6- [4-(3, 4-dimethoxybenzoyl)-1-piperazinyl] -2 (1H)-quinolinone, a new oral inotropic agent, wascarried out in 6 healthy Japanese malevolunteers. A double-blind test was performed to evaluate the safety, the pharmacodynamics, and the hemodynamic action with oral administration of a placebo, 30 mg and 60 mg of OPC-8212. The tolerance and the pharmacokinetic profile were also studied by oral administrationof 480 mg of OPC-8212. No pronounced change was noted in vital signs (bloodpressure and pulse rate). Echocardiographic study showed a decrease of the left ventricularendo-systolic dimension without change of the left ventricular end diastolic dimensionand an increase of the left ventricular ejection fraction. Mechanocardiograms showed ashortening of the left ventricular ejection time. No abnormalities were found in therespiratory system, the digestive system, or the laboratory data. The maximum concentrationincreased nonlinearly, increasing with dosage, peak time (T<SUB>max</SUB>) was about 4 to 8 hr.In conclusion, OPC-8212 has an inotropic action without chronotropic and arrhythmogenicaction, andhad no side effects in healthy volunteers.
一般社団法人日本臨床薬理学会の論文