Autism spectrum disorders (ASD) refer to a group of neuro-developmental disorders affecting young children and adults. Currently, the treatment options for ASD are mostly restricted to treating its symptoms. Among the various approaches for treating ASD, pharmacobiology-based treatments are numerous. Our objective is to review the up-to-date information on different types of medications and briefly discuss the evidence-based potential of these treatments in ASD therapy. PubMed searches for reports and reviews on clinical data from the last 15 years, between 2002-2017, using search terms of each category of treatment along with the terms “autism”, “mechanism”, and/or “side effects” were conducted. Several pharmacobiological interventions have been prescribed for ASD, including antipsychotics, stimulants, antidepressants, supplements, and special diets. However, none of these methods is an effective ASD treatment, and only few show much promise. We provide a brief overview of the current pharmacobiological treatments for ASD, their mechanisms of action, and clinical research-based evidence on their effectiveness. Based on our review, we recommend that caution should be exercised when choosing a pharmacobiological treatment method for ASD as majority of existing evidence is not from large-scale long-term high quality studies.Future research should focus on rigorous investigative design, long-term implementation, and meaningful uniform outcome measurements.