オランザピンは非常に有効な抗精神病薬ですが、著しい体重増加や代謝への影響といったリスクにより、その使用には制限があります。A combination of olanzapine and the opioid receptor antagonist samidorphan (OLZ/SAM) was recently approved in the United States for the treatment of adults with schizophrenia and bipolar I disorder. OLZ/SAM provides the antipsychotic efficacy of olanzapine while mitigating olanzapine-associated weight gain through opioid-receptor blockade. Physiologically-based pharmacokinetic (PBPK) modeling was used to assess the drug-drug interaction (DDI) potential of OLZ/SAM as well as to inform dosing in special populations, including smokers and those with organ impairment. The focus of the presentation was on leveraging PBPK modeling during the development of OLZ/SAM and regulatory interactions.