title: HIV-chemotherapy and -prophylaxis: new drugs, leads and approaches.
abstract: In recent years, significant progress has been made towards the chemotherapy (and prophylaxis) of HIV infections. This progress is situated at three different levels. (i) New anti-HIV drugs have been approved for clinical use and have entered the market: the virus entry inhibitor enfuvirtide (Fuzeon), the nucleoside reverse transcriptase inhibitor (NRTI) emtricitabine (Emtriva), the nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir disoproxil fumarate (Viread trade mark ) and the HIV protease inhibitor (PI) atazanavir (Reyataz trade mark ). (ii) Other compounds have proceeded through preclinical and/or clinical development: CXCR4 antagonists (i.e. AMD070), CCR5 antagonists (i.e. SCH-C), NRTIs (such as amdoxovir), NNRTIs (such as etravirine), integrase inhibitors (such as S-1360) and PIs (such as tipranavir). (iii) Yet other compounds, acting by novel mechanisms, have recently been identified as anti-HIV agents that seem worthy of further (pre)clinical development: cell receptor CD4 down-modulators (i.e. cyclotriazadisulfonamides), viral envelope gp120-binding agents such as plant lectins and glycopeptide antibiotics, HIV integrase inhibitors such as the pyranodipyrimidine V-165, and two new classes of compounds (i.e. N-aminoimidazoles and pyridine oxide derivatives) which seem to interfere with a post-integration, transcription transactivation event. Taken together, it is obvious that the approaches for the treatment of HIV infections in recent years have become both more diverse and more efficient.
authors.affiliation: Rega Institute for Medical Research, K.U. Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium. erik.declercq@rega.kuleuven.ac.be
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D015704:CD4 Antigens / Q000187:drug effects / Q000378:metabolism; D018890:Chemoprevention / Q000379:methods; D015536:Down-Regulation; D015699:HIV Envelope Protein gp120 / Q000187:drug effects / Q000378:metabolism; D015658:HIV Infections / Q000188:drug therapy* / Q000517:prevention & control*; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008969:Molecular Sequence Data; D009705:Nucleosides / Q000737:chemistry / Q000494:pharmacology; D009711:Nucleotides / Q000737:chemistry / Q000494:pharmacology; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D019428:HIV Integrase Inhibitors; D017320:HIV Protease Inhibitors; D009705:Nucleosides; D009711:Nucleotides; D019718:Receptors, CXCR4; D018894:Reverse Transcriptase Inhibitors