Zika virus (ZIKV) is a mosquito-borne flavivirus associated with neurological complications such as Limbari syndrome in adults and microcephaly in newborns. As there are no drugs or preventive vaccines available to specifically treat ZIKV infection, there is an urgent need to take comprehensive measures to prevent and control ZIKV infection and stop its spread. In this paper, we reviewed the structure and function of ZIKV gene and protein, and summarized the progress in the development of virus-targeting anti-ZIKV drug candidates through high-throughput screening and drug relocation, and summarized the mechanism of action of virus and host cell targeting drug candidates. The research and development trend of small molecule antiviral drugs in the future is prospected, which provides reference for promoting the research and development of new anti-ZIKV drugs.