Interoception is the sense of the physiological condition of the body. Recent studies suggested that interoception is involved in drug addiction and insular cortex is a key anatomical position. The neural mechanisms underlying such phenomena attract growing attention. In an effort to develop working hypotheses for future investigation, the article first reviewed the evidence of interoceptive regulation of addiction, and subsequently presented human and animal data that suggest a central role of the insular cortex in mediating interoception and addiction. On this basis, we proposed potential neurobiological mechanisms through which insular cortex may mediate drug addiction. Further, possible functional roles of neurotransmitters in the insular cortex are discussed in the context of drug addiction.