Role of integrase inhibitors in the treatment of HIV disease.
The introduction of highly active antiretroviral therapy (HAART) has produced a dramatic reduction in HIV-related mortality and morbidity among populations with widespread access to drugs. However, the increase in mutated HIV strains with reduced susceptibility to antiretroviral agents and the emergence of HAART-related side effects make it necessary to develop novel compounds characterized by activity against resistant viruses, a high genetic barrier to resistance and favorable pharmacokinetic and toxicity profiles. Integrase is a key enzyme in the life cycle of HIV and has represented an appealing target of antiretroviral therapy for several years. In 2006, after more than a decade of advances, pitfalls and disappointments, large clinical trials with integrase inhibitors in HIV-positive subjects have eventually begun.
Palmisano
Lucia
L
Istituto Superiore di Sanità, Department of Drug Research and Evaluation, Viale Regina Elena 299, 00161 Rome, Italy. l.palmisano@iss.it
D023241:Antiretroviral Therapy, Highly Active / Q000379:methods; D015658:HIV Infections / Q000188:drug therapy* / Q000201:enzymology; D019428:HIV Integrase Inhibitors / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006801:Humans
D019428:HIV Integrase Inhibitors