To Apply Microdosing or Not? Recommendations to Single Out Compounds with Non-Linear Pharmacokinetics

Non-linearities occur no more frequently between microdose and therapeutic dose studies than in therapeutic range ascending-dose studies. Most non-linearities are due to known saturable processes, and can be foreseen by integrating commonly available preclinical data. The guidance presented here may support decision making on incorporating a microdosing study in drug development