Nucleotide Reverse Transcriptase Inhibitors: A Thorough Review, Present Status and Future Perspective as HIV Therapeutics

Curr HIV Res. 2017;15(6):411-421. doi: 10.2174/1570162X15666171120110145.

Abstract

Background: Human immunodeficiency virus type-1 (HIV-1) infection leads to acquired immunodeficiency syndrome (AIDS), a severe viral infection that has claimed approximately 658,507 lives in the US between the years 2010-2014. Antiretroviral (ARV) therapy has proven to inhibit HIV-1, but unlike other viral illness, not cure the infection.

Objective: Among various Food and Drug Administration (FDA)-approved ARVs, nucleoside/ nucleotide reverse transcriptase inhibitors (NRTIs) are most effective in limiting HIV-1 infection. This review focuses on NRTIs mechanism of action and metabolism.

Methods: A search of PubMed (1982-2016) was performed to capture relevant articles regarding NRTI pharmacology.

Results: The current classical NRTIs pharmacology for HIV-1 prevention and treatment are presented. Finally, various novel strategies are proposed to improve the efficacy of NRTIs, which will increase therapeutic efficiency of present-day HIV-1 prevention/treatment regimen.

Conclusion: Use of NRTIs will continue to be critical for successful treatment and prevention of HIV-1.

Keywords: AIDS; Antiretroviral drugs; HIV-1; NRTIs; antiretroviral therapy; nanomedicine.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy
  • Acquired Immunodeficiency Syndrome / virology
  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / therapeutic use*
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism
  • HIV Infections / virology*
  • HIV-1 / drug effects*
  • Humans
  • Metabolic Networks and Pathways / drug effects
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Nucleotides / metabolism
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Treatment Outcome

Substances

  • Anti-HIV Agents
  • Nucleotides
  • Reverse Transcriptase Inhibitors