Antiretroviral therapy

03:20 EDT 26th August 2019 | BioPortfolio

Standard antiretroviral therapy (ART) consists of the combination of at least three antiretroviral (ARV) drugs to maximally suppress the HIV virus and stop the progression of HIV disease. Huge reductions have been seen in rates of death and suffering when use is made of a potent ARV regimen, particularly in early stages of the disease.

ART are medications that treat HIV. The drugs do not kill or cure the virus. However, when taken in combination they can prevent the growth of the virus. When the virus is slowed down, so is HIV disease. Antiretroviral drugs are referred to as ARV. Combination ARV therapy (cART) is referred to as highly active ART(HAART).


Each type, or “class”, of ARV drugs attacks HIV in a different way. The first class of anti-HIV drugs was the nucleoside reverse transcriptase inhibitors (also called NRTIs or “nukes”.) These drugs block step 4, where the HIV genetic material is used to create DNA from RNA. The following drugs in this class are used:

• Zidovudine (Retrovir, AZT)
• Didanosine (Videx, Videx EC, ddI)
• Stavudine (Zerit, d4T)
• Lamivudine (Epivir, 3TC)
• Abacavir (Ziagen, ABC)
• Tenofovir, a nucleotide analog (Viread, TDF)
• Combivir (combination of zidovudine and lamivudine)
• Trizivir (combination of zidovudine, lamivudine and abacavir)
• Emtricitabine (Emtriva, FTC)
• Truvada (combination of emtricitabine and tenofovir)
• Epzicom (combination of abacavir and lamivudine)

Non-nucleoside reverse transcriptase inhibitors, also called non-nukes or NNRTIs, also block step 4 but in a different way. Five have been approved:

  • Efavirenz (Sustiva or Stocrin, EFV, also part of Atripla)
  • Etravirine (Intelence, ETR)• Rilpivirine (Edurant, RPV, also part of Complera or Epivlera)
  • Delavirdine (Rescriptor, DLV)
  • Nevirapine (Viramune, NVP)

Protease inhibitors or PIs block Step 10, where the raw material for new HIV virus is cut into specific pieces. Ten protease inhibitors are approved:

  • Amprenavir (Agenerase, APV)
  • Atazanavir (Reyataz, ATZ)
  • Darunavir (Prezista, DRV)
  • Fosamprenavir (Lexiva, Telzir, FPV)
  • Indinavir (Crixivan, IDV)
  • Lopinavir/ritonavir (Kaletra or Aluvia, LPV/RTV)
  • Nelfinavir (Viracept, NFV)
  • Ritonavir (Norvir, RTV)
  • Saquinavir (Invirase, SQV)
  • Tipranavir (Aptivus, TPV)

Entry inhibitors prevent HIV from entering a cell by blocking step 2 of the life cycle. Two drugs of this type have been approved:

  • Enfuvirtide (Fuzeon, ENF, T-20)
  • Maraviroc (Selzentry or Celsentri, MVC)

HIV integrase inhibitors prevent HIV from inserting its genetic code into the human cell's code in step 5 of the life cycle. The two drugs of this type are:

  • Elvitegravir (EVG, part of the combination Stribild)
  • Dolutegravir (Tivicay, DTG)
  • Raltegravir (Isentress, RAL)


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