OBJECTIVES: To determine etravirine concentrations in CSF in HIV-infected patients. METHODS: Twelve HIV-1 adult antiretroviral-experienced patients receiving an etravirine-containing regimen for at least 1 month were enrolled. Both CSF and blood samples were taken around 12 h after the last etravirine dose. Liquid chromatography-tandem mass spectrometry was used to determine etravirine concentrations, and HIV-1 viral load was determined by real-time PCR (limit of detection 40 copies/mL). RESULTS: Twelve blood and 12 CSF samples were collected. The median CD4 count was 333 (84-765) cells/mm(3) and the median plasma HIV-1 viral load was <40 (range <40-1777) copies/mL. The median time on etravirine was 34 (range 4-140) weeks. The median etravirine concentration in plasma was 611.5 (range 148-991) ng/mL. The median CSF etravirine concentration was 7.24 (range 3.59-17.9) ng/mL; in all cases, values were above the IC(50) range (0.39-2.4 ng/mL). The median etravirine CSF:plasma ratio was 0.01 (range 0.005-0.03). The CSF viral load was >40 copies/mL in one patient and plasma viral load was still detectable after 4 weeks of therapy. CONCLUSIONS: Etravirine achieves concentrations several times greater than the IC(50) range in CSF. All patients with undetectable plasma viral load were virologically suppressed in CSF while receiving an etravirine-containing regimen. Etravirine may help in controlling HIV-1 in CNS.
OBJECTIVES: To determine etravirine concentrations in CSF in HIV-infectedpatients. METHODS: Twelve HIV-1 adult antiretroviral-experienced patients receiving an etravirine-containing regimen for at least 1 month were enrolled. Both CSF and blood samples were taken around 12 h after the last etravirine dose. Liquid chromatography-tandem mass spectrometry was used to determine etravirine concentrations, and HIV-1 viral load was determined by real-time PCR (limit of detection 40 copies/mL). RESULTS: Twelve blood and 12 CSF samples were collected. The median CD4 count was 333 (84-765) cells/mm(3) and the median plasma HIV-1 viral load was <40 (range <40-1777) copies/mL. The median time on etravirine was 34 (range 4-140) weeks. The median etravirine concentration in plasma was 611.5 (range 148-991) ng/mL. The median CSFetravirine concentration was 7.24 (range 3.59-17.9) ng/mL; in all cases, values were above the IC(50) range (0.39-2.4 ng/mL). The median etravirineCSF:plasma ratio was 0.01 (range 0.005-0.03). The CSF viral load was >40 copies/mL in one patient and plasma viral load was still detectable after 4 weeks of therapy. CONCLUSIONS:Etravirine achieves concentrations several times greater than the IC(50) range in CSF. All patients with undetectable plasma viral load were virologically suppressed in CSF while receiving an etravirine-containing regimen. Etravirine may help in controlling HIV-1 in CNS.
Authors: Anh Nguyen; Steven Rossi; David Croteau; Brookie M Best; David Clifford; Ann C Collier; Benjamin Gelman; Christina Marra; Justin McArthur; J Allen McCutchan; Susan Morgello; David Simpson; Ronald J Ellis; Igor Grant; Edmund Capparelli; Scott Letendre Journal: J Antimicrob Chemother Date: 2013-01-20 Impact factor: 5.790
Authors: R Gagliardini; M Fabbiani; S Fortuna; E Visconti; P Navarra; R Cauda; M Colafigli; A De Luca; E M Trecarichi; S Di Giambenedetto Journal: Infection Date: 2014-02-15 Impact factor: 3.553