Effects
Reverse transcriptase inhibitors (ATC J05AF) have antiviral properties against HIV. The effects are due to inhibition of the viral enzyme reverse transcriptase, which transcribes viral RNA into DNA and is important for viral replication.
Structure and properties
Within the drug group, two distinct classes are distinguished. The so-called nucleoside reverse transcriptase inhibitors, abbreviated NRTIs, are prodrugs that are phosphorylated in cells like the natural substrates and are thus activated. They are competitively incorporated into DNA as incorrect building blocks and lead to chain termination. The non-nucleoside reverse transcriptase inhibitors, the NNRTIs, do not require activation. As inhibitors, they bind to the enzyme’s active site, impeding its function.
Indications
- For treatment of infection with HIV as part of combination antiretroviral therapy (HAART). Some RTIs are also used to treat chronic hepatitis B. This article refers to HIV.
- HIV pre-exposure prophylaxis (see there).
Agents
Nucleoside reverse transcriptase inhibitors (NRTIs):
- Abacavir (Ziagen).
- Didanosine (Videx)
- Emtricitabine (Emtriva)
- Lamivudine (3TC)
- Stavudine (Zerit)
- Tenofovirdisoproxil (Viread)
- Tenofoviralafenamide (Vemlidy).
- Zidovudine (Retrovir AZT) – 1st HIV drug, 1987.
- Zalcitabine (not commercially available in many countries).
Non-nucleoside reverse transcriptase inhibitors (NNRTIs):
- Efavirenz (Stocrin).
- Etravirine (Intelence)
- Nevirapine (Viramune)
- Rilpivirine (Edurant)
- Delavirdine (not commercially available in many countries).
- Doravirin (Pifeltro)
