Tripterygium wilfordii Hook. F. (TwHF) is of traditional Chinese medicine in China. Because of its strong anti-inflammatory, immunosuppressive, and podocyte-protective effects, it has been widely used in various primary and secondary kidney diseases, especially in the clinical treatment of difficult refractory nephrotic syndrome, such as membranous nephropathy, focal segmental glomerulosclerosis, diabetic nephropathy, anaphylactoid purpura nephritis, and lupus nephritis, etc, showing remarkably unique advantages. However, there are still many clinical doctors with a large deviation in the understanding of the drug: avoiding use of it in fear of its toxicity, or pursuing efficacy without careful monitoring, which affect the correct use of the drug. Therefore, understanding TwHF's pharmacological and toxic effects, and grasping the correct preventive measures and reasonable application methods, will help reduce adverse drug reactions and give full play to its clinical efficacy.