A liquid chromatography-tandem mass spectrometric (LC-MS-MS) method for the highly sensitive determination of a new bone-anabolic agent, TAK-778 in human serum was developed. The internal standard (I.S.) used was deuterated TAK-778. TAK-778 and I.S. were extracted from serum samples with diethyl ether at neutral pH. A turbo ion spray interface was used as the ion source of LC-MS-MS, and the analysis was performed in the selected reaction monitoring mode. The lower limit of quantification was 0.02 ng/ml when 0.4 ml of serum was used, and the standard curve was linear in the range of 0.02-10 ng/ml. The method was precise; the intra- and inter-day precision of the method was not more than 17.9%. The accuracy of the method was good with the deviations between added and calculated concentration of TAK-778 being typically within 9.0%.