Acupuncture therapy combined with medication has been widely used in clinic practice in China and proved to be effective in the, treatment of many disorders. The authors of the present paper review researches on the underlying mechanism of joint application of acupuncture therapy and medication in recent decade from (1) neural regulation, (2) endocrine regulation, and (3) immunological regulation. After comprehensive analysis, the authors think that the mechanism underlying the enhanced clinical efficacy of acupuncture therapy combined with drugs may be closely associated with the following factors: (1) acupuncture stimulation of acupoints leads to changes of the drug concentration in the blood and/or in the target organ and, (2) the reactivity or sensitivity of the target organ tissues to the specifically effective drug elements is enhanced.