Reverse transcriptase inhibitor

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Reverse transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV infection. RTIs inhibit activity of reverse transcriptase, a viral enzyme that HIV needs to reproduce.

When a retrovirus infects a cell, reverse transcriptase transcribes the viral RNA onto the host cell's DNA. The host's own processes then reproduce the virus. RTIs block reverse transcriptase from transcribing retroviral genetic information onto a host cell's DNA, thus preventing HIV from multiplying.

RTIs come in three forms:

  • Nucleoside analog reverse transcriptase inhibitors (NARTIs or NRTIs)
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
  • Nucleotide analog reverse transcriptase inhibitors (NtARTIs or NtRTIs)

Nucleoside analog reverse transcriptase inhibitors

Nucleoside analog reverse transcriptase inhibitors (NARTIs or NRTIs) compose the first class of antiretroviral drugs developed.

Zidovudine 
Zidovudine, also called AZT, ZDV, and azidothymidine, has the trade name Retrovir®.
Didanosine 
Didanosine, also called ddI, with the trade names Videx® and Videx EC®, was the second FDA-approved antiretroviral drug.
Zalcitabine 
Zalcitabine, also called ddC and dideoxycytidine, has the trade name Hivid®.
Stavudine 
Stavudine, also called d4T, has trade names Zerit® and Zerit XR®.
Lamivudine 
Lamivudine, also called 3TC, has the trade name Epivir®.
Abacavir 
Abacavir, also called ABC, has the trade name Ziagen®, is an analog of guanosine.
Emtricitabine 
Emtricitabine, also called FTC, has the trade name Emtriva® (formerly Coviracil).

Non-nucleoside reverse transcriptase inhibitors

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) compose the third class of antiretroviral drugs that were developed. In all cases, patents remain in force until beyond 2010.

Nevirapine 
Nevirapine has the trade name Viramune®.
Delavirdine 
Delavirdine has the trade name: Rescriptor®. It was approved by the FDA April 4, 1997 and is thus the eleventh approved antiretroviral. It is now rarely used, as it has no advantages and several disadvantages compared with Nevirapine or Efavirenz.
Efavirenz 
Efavirenz has trade names Sustiva® and Stocrin®.

Nucleotide analog reverse transcriptase inhibitors

Normally, nucleoside analogs are converted into nucleotide analogs by the body. Taking Nucleotide Analog Reverse Transcriptase Inhibitors (NtARTIs or NtRTIs) directly allows conversion steps to be skipped, causing less toxicity.

Tenofovir 
Tenofovir, also known as tenofovir disoproxil fumarate, has the trade name Viread®.
Adefovir 
Adefovir, also known as bis-POM PMPA, has trade names Preveon® and Hepsera®. It is not approved by the FDA for treatment of HIV.