Small molecule drugs, especially anti-tumor drugs, generally have defects such as poor water solubility, short half-life, poor targeting of biological tissue distribution and high toxicity, which greatly limit their clinical applications. PEGylated small molecule drugs can significantly improve the water solubility of drug molecules and in vivo pharmacokinetic parameters, as well as reduce their toxic and side effects, which makes many small molecule drugs with significant curative effects but limited in clinical applications have new development prospects.