Abstract: Reverse transcriptase (RT), which reverse-transcribes viral single-stranded RNA into double-stranded DNA, plays an irreplaceable role in the replication cycle of human immunodeficiency virus type 1 (HIV-1). Reverse transcriptase inhibitors (RTIs), a key component of highly active antiretroviral therapy (HAART), have achieved great success in the treatment of AIDS, drastically reducing the morbidity and mortality of HIV-infected patients. However, with the long-term application of RTIs in clinic, many problems, such as drug resistance and adverse reaction, have gradually emerged. Therefore, it is of great significance to develop novel HIV-1 RTIs with high efficiency, low toxicity and anti-drug resistance. In this review, the latest research progress of anti-AIDS drugs and related drug candidates targeting HIV-1 RT in the past three years is summarized, aiming to provide some reference for further research and development of novel RTIs.