Background:

Zidovudine is an inhibitor of the reverse transcriptase of HIV-1[1].

Zidovudine is the first effective agent for the management of HIV-1 infection and is approved by FDA as a drug for AIDs in 1987. As a nucleoside analogue, zidovudine inhibits the activity of the reverse transcriptase with its triphosphate structure. In the in vitro studies, zidovudine shows strong inhibition of HIV-1 replication and the cytopathic effect of the virus. The addition of 5μM and 10μM zidovudine completely protects TM3 cells (a normal IL-2-dependent helper/inducer T-cell clone) and ATH8 cells against the cytopathic effect of HIV. It exhibits complete inhibition of reverse transcriptase at concentration up to 0.5μM. However, the resistance of zidovudine has been found in vitro and in vivo since 1989 [1, 2].

参考文献:
[1] Mitsuya H, Weinhold K J, Furman P A, et al. 3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proceedings of the National Academy of Sciences, 1985, 82(20): 7096-7100.
[2] McLeod G X, Hammer S M. Zidovudine: five years later. Annals of internal medicine, 1992, 117(6): 487-501.