The oxygen (OPAHs), nitro (NPAHs), hydroxyl (OH-PAHs), and alkylated (APAHs) derivatives of polycyclic aromatic hydrocarbon (PAHs) are ubiquitous pollutants in the environment. The concentrations of NPAHs, OPAHs, OH-PAHs, and APAHs are lower than that of PAHs in the environment, but the carcinogenic abilities of the derivatives are usually 10 to 1,000-fold higher than that of parent PAHs. There are three main pathways for the exposure of polycyclic aromatic compounds to humans, including inhalation, direct contact, and ingestion. After exposure by inhalation, they are mainly distributed in the lungs, affecting lung function and causing inflammation, asthma, etc. Due to the digestive system's strong capacity for metabolism, intake of PAHs and the derivatives is primarily distributed in the digestive system and metabolized there. And it may lead to dysplasia of these organs and even to cancer. The skin is the primary site of direct contact with PAH derivatives. PAH derivatives can enter the bloodstream through all three contact pathways, thereby accumulating in various organs. This study aimed to summarize the influence of exposure pathways on tissue distribution and the health impact of PAH derivatives to provide references for future research and evaluation on public health.