New developments in anti-HIV chemotherapy

Farmaco. Jan-Feb 2001;56(1-2):3-12. doi: 10.1016/s0014-827x(01)01007-2.


Virtually all the compounds that are currently used, or under advanced clinical trial, for the treatment of HIV infections, belong to one of the following classes: (i) nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): i.e. zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, emtricitabine, tenofovir (PMPA) disoproxil fumarate; (ii) non-nucleoside reverse transcriptase inhibitors (NNRTIs): i.e. nevirapine, delavirdine, efavirenz, emivirine; and (iii) protease inhibitors (PIs): i.e. saquinavir, ritonavir, indinavir, nelfinavir and amprenavir. In addition, various other events in the HIV replicative cycle are potential targets for chemotherapeutic intervention: (i) viral adsorption, through binding to the viral envelope glycoprotein gp120; (ii) viral entry, through blockade of the viral coreceptors CXCR4 and CCR5; (iii) virus-cell fusion; (iv) viral assembly and disassembly; (v) proviral DNA integration; (vi) viral mRNA transcription. Also, new NRTIs, NNRTIs and PIs have been developed that possess respectively improved metabolic characteristics, or increased activity against NNRTI-resistant HIV strains or, as in the case of PIs, a different, non-peptidic scaffold. Given the multitude of molecular targets with which anti-HIV agents can interact, one should be cautious in extrapolating from cell-free enzymatic assays to the mode of action of these agents in intact cells.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • HIV / drug effects
  • HIV / genetics
  • HIV Envelope Protein gp120 / drug effects
  • HIV Protease Inhibitors / pharmacology
  • Integrases / drug effects
  • Receptors, CXCR4 / antagonists & inhibitors
  • Reverse Transcriptase Inhibitors / pharmacology
  • Transcription, Genetic / drug effects
  • Zinc Fingers


  • Anti-HIV Agents
  • HIV Envelope Protein gp120
  • HIV Protease Inhibitors
  • Receptors, CXCR4
  • Reverse Transcriptase Inhibitors
  • Integrases