Raltegravir.
* Raltegravir, the first in a new class of orally administered HIV type-1 (HIV-1) integrase inhibitors, selectively inhibits the strand transfer activity of HIV-1 and its integration into human DNA, a key stage in retroviral propagation, thereby limiting viral replication and the infection of new cells. * In two randomized, double-blind (with in-house blinding), placebo-controlled, multicentre, ongoing phase III trials, the proportion of patients achieving HIV-1 RNA loads of <400 copies/mL (primary endpoint) was significantly greater in raltegravir plus optimized background therapy (OBT) recipients than in placebo plus OBT recipients (preliminary 24-week results). * The proportion of patients achieving viral loads of <50 copies/mL was significantly greater with raltegravir plus OBT than with placebo plus OBT in the two studies. * In addition, mean CD4+ cell counts (secondary endpoint) were significantly increased from baseline in patients receiving raltegravir plus OBT relative to those receiving placebo plus OBT. * Raltegravir therapy was well tolerated overall. The incidence of mild to moderate adverse events was similar in the raltegravir and placebo arms of the two randomized trials.
Croxtall
Jamie D
JD
Wolters Kluwer Health | Adis, Auckland, New Zealand. demail@adis.co.nz
Lyseng-Williamson
Katherine A
KA
Perry
Caroline M
CM
D000284:Administration, Oral; D004334:Drug Administration Schedule; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development; D006801:Humans; D009930:Organic Chemicals / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D016896:Treatment Outcome
D019428:HIV Integrase Inhibitors; D009930:Organic Chemicals; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium