Determining the antiviral activity of tenofovir disoproxil fumarate in treatment-naive chronically HIV-1-infected individuals.
OBJECTIVE
To assess the efficacy of tenofovir disoproxil fumarate (TDF) monotherapy by following the initial rate of decline in plasma viral load, which is a measure of the efficacy of therapy in blocking viral replication.


METHODS
An open-label, single-site study of TDF monotherapy in 10 antiretroviral drug-naive chronically HIV-1-infected individuals.


METHODS
Antiviral responses were assessed at baseline and during 21 days of monotherapy with TDF by measuring plasma HIV-1 RNA levels. The rate of change in HIV-1 RNA from baseline was determined both by linear regression and by fitting to a published model. Slopes were compared with those previously determined for ritonavir monotherapy.


RESULTS
Over 21 days, mean plasma HIV-1 RNA levels in the TDF-treated patients fell 1.5 log(10) copies/ml (range, 0.7-2.0). The initial rates of decline in plasma HIV-1 RNA in the 10 TDF-treated patients and in 25 protease inhibitor-naive subjects treated with ritonavir monotherapy were nearly identical.


CONCLUSIONS
The reduction in plasma HIV-1 RNA with TDF monotherapy was comparable with the decline observed in previous studies of protease inhibitor monotherapy. TDF is a potent antiretroviral agent and has comparable inherent antiviral activity with that of ritonavir, a potent protease inhibitor. These data support further study of TDF-based regimens in simplified combinations of antiviral agents as initial treatment for chronic HIV-1 infection.
Louie
Michael
M
Aaron Diamond AIDS Research Center, Rockefeller University, New York, NY 10016, USA.
Hogan
Christine
C
Hurley
Arlene
A
Simon
Viviana
V
Chung
Chris
C
Padte
Neal
N
Lamy
Patrick
P
Flaherty
John
J
Coakley
Dion
D
Di Mascio
Michele
M
Perelson
Alan S
AS
Markowitz
Martin
M
D000225:Adenine / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D000328:Adult; D019380:Anti-HIV Agents / Q000627:therapeutic use*; D002908:Chronic Disease; D005260:Female; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000302:isolation & purification*; D006801:Humans; D008297:Male; D008875:Middle Aged; D063065:Organophosphonates; D009943:Organophosphorus Compounds / Q000627:therapeutic use*; D011355:Prodrugs / Q000627:therapeutic use*; D012367:RNA, Viral / Q000097:blood; D018894:Reverse Transcriptase Inhibitors / Q000627:therapeutic use; D000068698:Tenofovir; D019562:Viral Load
D019380:Anti-HIV Agents; D063065:Organophosphonates; D009943:Organophosphorus Compounds; D011355:Prodrugs; D012367:RNA, Viral; D018894:Reverse Transcriptase Inhibitors; D000068698:Tenofovir; D000225:Adenine