Efficacy and Safety 48 Weeks after Switching from Efavirenz to Rilpivirine Using Emtricitabine/Tenofovir Disoproxil Fumarate–Based Single-Tablet Regimens

Abstract

Switching from EFV/FTC/TDF to RPV/FTC/ TDF was a safe, efficacious option for virologically suppressed HIV-infected patients with EFV intolerance wishing to remain on an STR.

Doravirine Suppresses Common Nonnucleoside Reverse Transcriptase Inhibitor-Associated Mutants at Clinically Relevant Concentrations

“…For DOR, at a daily dose of 100 mg (the dose employed in the phase 3 clinical trials), the plasma trough concentration at 24 h is 830 nM. The trough concentrations of EFV and RPV are 5,600 nM and 260 nM at 24 h at clinical doses of 600 mg and 25 mg, respectively (18,19). These values and the respective IC 50 s determined in the presence of 100% serum were used to calculate IQs for each of these drugs versus the panel of NNRTI mutants, as shown in Fig.…”

Gestione del rischio cardiovascolare nel paziente HIV positivo

“…Nell'ambito degli inibitori nucleosidici/nucleotidici della transcriptasi inversa (NRTI), i dati della letteratura hanno evidenziato generalmente una riduzione dei valori di trigliceridi, colesterolo totale ed LDL sostituendo stavudina, didanosina o zidovudina con tenofovir (preferibile) o abacavir (in alternativa, se il test HLA B*5701 è negativo) (24,25). Tra gli inibitori non nucleosidici della transcriptasi inversa (NNRTI), efavirenz è associato più spesso a dislipidemia e può essere sostituito, con effetti favorevoli sui parametri lipidici, da altri NNRTI (quali nevirapina, etravirina o rilpivirina) o da un inibitore dell'integrasi (raltegravir) (26)(27)(28)(29)(30). Gli inibitori della proteasi boosterati con ritonavir (PI/r) sono i farmaci più spesso associati a ipertrigliceridemia e/o ipercolesterolemia e gli studi di switch hanno dimostrato che si può ottenere un miglioramento significativo della dislipidemia sostituendo il PI/r con un altro PI a minor impatto sull'assetto lipidico (atazanavir, atazanavir/r, darunavir/r), con un NNRTI (nevirapina, etravirina, rilpivirina) o con un inibitore dell'integrasi (raltegravir, elvitegravir/cobicistat) (31-39).…”

Emtricitabine/rilpivirine/tenofovir disoproxil fumarate single-tablet regimen in HIV-1 infection: a guide to its use in the EU

“…Consistent with STaR, all patients in a smaller trial (Study 111; n = 49) who were already virologically suppressed with the emtricitabine/efavirenz/tenofovir DF single-tablet regimen, but wished to change their regimen because of efavirenz intolerance, sustained a viral load of \50 copies/mL 12 weeks after switching to the emtricitabine/rilpivirine/tenofovir DF single-tablet regimen [8,13] or full analysis set [11,12], using the time-to-loss-of-virological response [8,13] or snapshot [11,12] algorithm for virological outcomes BL baseline, EFV efavirenz, FTC emtricitabine, pts patients, RPV rilpivirine, TDF tenofovir disoproxil fumarate a Pts received FTC/RPV/TDF 200 mg/25 mg/300 mg or FTC/EFV/TDF 200 mg/600 mg/300 mg as once-daily single-tablet regimens in STaR, and RPV 25 mg or EFV 600 mg once daily in combination with FTC/TDF in ECHO and THRIVE b Primary endpoint at week 48 c 95 % confidence interval for the difference between the RPV group and comparator group d RPV regimen was noninferior to the EFV regimen, based on a noninferiority margin of 12 % for the between-regimen difference e Statistical analysis for between-group difference was not reported (primary endpoint), with most patients continuing to sustain this degree of suppression up to 48 weeks (Table 3) [30,31]. At 48 weeks, no significant change in CD4?…”

“…cell count was evident and fewer than 5 % of patients experienced virological failure (Table 3). Most patients (92 %) were C95 % adherent through week 48, as measured by pill count [30].…”

“…The adverse reactions most frequently associated with rilpivirine (incidence C2 %, grades 2-4) include depressive disorders, insomnia and headache, and those most Table 3 Efficacy of switching to the oral once-daily emtricitabine/rilpivirine/tenofovir disoproxil fumarate single-tablet regimen in virologically-suppressed, treatment-experienced adults with HIV-1 infection in phase IIb (noncomparative) [30] Week 24 100…”