Provided are methods for improving the pharmacokinetics of drug therapy. In one aspect methods are provided for co-administration of a liposomally encapsulated, PEGylated, or protein-conjugated drug via a parenteral route and the same drug in free (non-encapsulated, PEGylated, or protein-conjugated) form via an enteral or parenteral route. In another aspect, methods are provided for treating a cancer in a patient by co-administering liposomal irinotecan and free irinotecan, optionally in further combination with additional therapeutic agents.本發明提供用於改善藥物治療之藥物動力學之方法。在一個態樣中,提供用於共投與經由非經腸路徑經脂質體囊封、聚乙二醇化或蛋白質結合藥物及經由腸內或非經腸路徑呈游離(非囊封、聚乙二醇化或蛋白質結合)形式之相同藥物的方法。在另一態樣中,提供藉由共投與脂質體伊立替康及游離伊立替康視情況進一步與其他治療劑的組合來治療患者之癌症的方法。