This 6-year-old boy has a birth history of preterm 30^(+2) weeks, birth body weight 1430 g, Apgar score 8 at birth and 9 at 5 minutes. The neonatal neurosonography revealed bilateral grade I intraventricular hemorrhage with mild ventriculomegaly and left periventricular cystic leukomalacia. The boy received a regular rehabilitation program and follow-up treatment in outpatient service of pediatric neurology. The boy had delays in cognitive, language, and motor development. In addition, the boy developed an extreme focus on the specific topic of interest and had difficulty with changes in routines for one year. As he was diagnosed with Asperger syndrome by a pediatric psychiatrist, the boy's parents hoped that he could receive treatment of Chinese medicine. According to TCM theory, the diagnosis was five kinds of maldevelopment with agitation, and the syndrome differentiation was deficiency of liver and kidney, stagnation of liver qi, and ascendant hyperactivity of liver yang. Through the treatment of Chinese herbal therapy in which Yi-Gan San as the main prescription and acupuncture, the boy's mood, communication skills, and cognitive function were significantly improved. This case report presented Chinese herbal therapy and acupuncture are effective in treating Asperger syndrome associated with delayed development.