Elvitegravir (GS9137) è un inibitore dell’integrasi sviluppato da Gilead. TMC 278 è un analogo non nucleosidico sviluppato da Tibotec.GS9137 ELVITEGRAVIR – Gilead Sciences. Studio di fase II (dose findings) su pazienti pre-trattati. 3 diversi dosaggi. Il farmaco appare potente.
Complementi in inglese
278 treatment-experienced patients received one of three doses of GS9137 or another regimen 70% of whom received tipranavir or TMC114. Patients had about 150 CD4s at baseline and 4.5 log viral load. Mean viral load declined by 1.2 log in the comparator arm and 1.7 log in the high dose GS9137 (125mg qd boosted with 100mg RTV) arm; the difference was statistically significant. 91% in the high dose integrase arm and 61%in the CPI arm achieved 1 log or more reduction in viral load, and 76% vs 51% achieved 2 logs or more; both were statistically significant. Of note, at week two the viral load reduction in the high dose integrase group was slightly more than 2 logs before rebounding because the background therapy was too weak showing that GS9137 appears to be potent. In fact at week 24 the mean decline in viral load was -2.1 log for patients on GS9137 if they were also taking 1 or more active nukes or first use Fuzeon compared to -0.7 log reduction for patients taking GS9137 without any active drugs in background. There did not appear to be any safety or adverse events issues.
TMC 278– Studio di fase II su pazienti naïve che mette a confronto questo nuovo farmaco della Tibotec con efavirenz. Interessante il profilo del farmaco.
Complementi in inglese
Phase II study comparing TMC278, a new NNRTI to efavirenz in treatment naives with CD4s of 200 and 70,000 viral load. At week 48, 80% in all 3 TMC278 dose arms and efavirenz had <50 copies/ml (ITT) and log reduction of 2.6 and CD4 increase of 130. TMC278 had a better CNS side effect profile: less dizziness, somnolecence, vertigo, abnormal dreams, rash; and a better lipid profile, very little or no change in total cholesterol, LDL-C, and triglycerides while efavirenz patients had better HDL improvement (+12 vs +5).The 75 mg dose has been selected. Phase III is expected to start later in the year and based on this development should take 2 years to be available.