title: The introduction of the fusion inhibitors in the HAART-regimens.
abstract: Interference with HIV entry into target cells provides a novel approach to the treatment of HIV infection. The inhibition of virus fusion with the co-receptor substrate seems the most specific and potentially best way to interfere with HIV infection and replication. The efficacy of the first compound available (enfuvirtide) is evident after the pre-registrative phase II and III studies showing also that the presence of anti gp 41 antibodies in the plasma of the treated patients does not interfere with drug activity. In the failing enfuvirtide treated patients resistant virus was detected in 7/7 after > one year of treatment with genotypic mutations in the HR env domain, however no interclass cross resistance was evidenced. Mutants selected in vivo demonstrated a slight reduction of replication capacity.
authors.affiliation: Vita Salute University, San Raffaele Scientific Institute, Clinic of Infectious Diseases, Milan.
authors.forename: H
authors.initials: H
authors.lastname: Hasson
authors.forename: A
authors.initials: A
authors.lastname: Castagna
authors.forename: M
authors.initials: M
authors.lastname: Clementi
authors.forename: S
authors.initials: S
authors.lastname: Menzo
authors.forename: A
authors.initials: A
authors.lastname: Danise
authors.forename: A
authors.initials: A
authors.lastname: Lazzarin
mesh_terms: D023241:Antiretroviral Therapy, Highly Active; D024882:Drug Resistance, Viral / Q000235:genetics; D000077560:Enfuvirtide; D015752:Genes, env; D006678:HIV / Q000187:drug effects*; D015483:HIV Antibodies / Q000097:blood; D015700:HIV Envelope Protein gp41 / Q000276:immunology / Q000494:pharmacology / Q000627:therapeutic use; D023581:HIV Fusion Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D006801:Humans; D008826:Microbial Sensitivity Tests; D010446:Peptide Fragments / Q000494:pharmacology / Q000627:therapeutic use; D014779:Virus Replication / Q000502:physiology
chemical_list: D015483:HIV Antibodies; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors; D010446:Peptide Fragments; D000077560:Enfuvirtide