A Randomized, Open-Label, Phase I Clinical Study of Dalpiciclib With Different Specifications After Process...

The purpose of this study was to determine the pharmacokinetic characteristics and safety of dalpiciclib at 100-, 125-, and 150-mg doses after process modification in healthy Chinese volunteers. This single-center, randomized, open-label, three-dose, phase I clinical study was conducted in healthy Chinese adults. Thirty-six volunteers were randomized to three groups, including groups administered 100, 125, and 150 mg of dalpiciclib, and each group contained an equal number of males and females. A single oral dose of dalpiciclib was administered to each group, and plasma concentrations were measured by a validated liquid chromatography-tandem mass spectrometry method. The oral formulation of dalpiciclib was well absorbed, the plasma concentration reached the maximum concentration (C_max ) in 4-6 hours, and it was eliminated from plasma with a mean terminal half-life of 42.9-45.5 hours after 100-150 mg was administered. Dalpiciclib exhibited safety and favorable pharmacokinetic profiles, supporting further investigations in phase II studies. The plasma exposure of dalpiciclib was dose-dependent, with increasing doses in the range of 100-150 mg.