In China,antithyroid drugs are the first choice of treatment for hyperthyroidism.However,their side effects may result in agranulocytosis,which has an insidious onset and requires urgent treatment.Up to date,the mechanisms of agranulocytosis caused by antithyroid drugs is still unclear.Herein,the article reviewed the direct toxic activities,the immune effects,and the genetic susceptibility of antithyroid drugs,which may be helpful to provide better clinical treatment options and improve the prognosis of agranulocytosis caused by the drugs.