[Reverse transcriptase inhibitors and the therapy of HIV infection]

Azidothymidine (retrovir) and didesoxyinosine, which represent nucleoside agents, are major remedies in the treatment of HIV infection and acquired immunodeficiency syndrome (AIDS). The paper describes the molecular mechanism of their action. It implicates that triphosphates of these nucleosides selectively suppress the activity of reverse transcriptase (RNA-dependent DNA polymerase) of HIV by a termination mechanism. This results in effective inhibition of HIV reproduction and recovery of lymphocyte count and yields marked therapeutical benefits. The new generation anti-HIV agents are nucleoside-based phosphonates which were discovered by Russian investigators in 1987. The agents having a significant anti-HIV activity are low toxic. Emphasis is made on combined therapy of HIV infection, which holds much promise.