Abstract
OBJECTIVE: TMC125-C223 is an open-label, partially blinded, randomized clinical trial to evaluate the efficacy and safety of two dosages of etravirine (TMC125), a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against wild-type and NNRTI-resistant HIV-1. DESIGN: A total of 199 patients were randomly assigned 2:2:1 to twice-daily etravirine 400 mg, 800 mg and control groups, respectively. The primary endpoint was a change in viral load from baseline at week 24 in the intention-to-treat population. METHODS: Patients had HIV-1 with genotypic resistance to approved NNRTIs and at least three primary protease inhibitor (PI) mutations. Etravirine groups received an optimized background of at least two approved antiretroviral agents [nucleoside reverse transcriptase inhibitors (NRTI) and/or lopinavir/ritonavir and/or enfuvirtide]. Control patients received optimized regimens of at least three antiretroviral agents (NRTIs or PIs and/or enfuvirtide). RESULTS: The mean change from baseline in HIV-1 RNA at week 24 was -1.04, -1.18 and -0.19 log10 copies/ml for etravirine 400 mg twice a day, 800 mg twice a day and the control group, respectively (P < 0.05 for both etravirine groups versus control). Etravirine showed no dose-related effects on safety and tolerability. No consistent pattern of neuropsychiatric symptoms was observed. There were few hepatic adverse events, and rashes were predominantly early onset and mild to moderate in severity. CONCLUSION: Etravirine plus an optimized background significantly reduced HIV-1-RNA levels from baseline after 24 weeks in patients with substantial NNRTI and PI resistance, and demonstrated a favorable safety profile compared with control.
| Original language | English |
|---|---|
| Journal | AIDS |
| Volume | 21 |
| Issue number | 6 |
| DOIs | |
| State | Published - Mar 1 2007 |
| Externally published | Yes |
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Keywords
- 24-week primary analysis
- Etravirine
- Non-nucleoside reverse transcriptase inhibitor
- Randomized trial
- Resistant HIV-1
- TMC125
ASJC Scopus subject areas
- Immunology and Allergy
- Immunology
Cite this
Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1 : Primary 24-week analysis. / Nadler, Jeffrey P.; Berger, Daniel S.; Blick, Gary; Cimoch, Paul J.; Cohen, Calvin J.; Greenberg, Richard N.; Hicks, Charles B.; Hoetelmans, Richard M W; Iveson, Kathy J.; Jayaweera, Dushyantha T; Mills, Anthony M.; Peeters, Monika P.; Ruane, Peter J.; Shalit, Peter; Schrader, Shannon R.; Smith, Stephen M.; Steinhart, Corklin R.; Thompson, Melanie; Vingerhoets, Johan H.; Voorspoels, Ellen; Ward, Douglas; Woodfall, Brian.
In: AIDS, Vol. 21, No. 6, 01.03.2007.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1
T2 - Primary 24-week analysis
AU - Nadler, Jeffrey P.
AU - Berger, Daniel S.
AU - Blick, Gary
AU - Cimoch, Paul J.
AU - Cohen, Calvin J.
AU - Greenberg, Richard N.
AU - Hicks, Charles B.
AU - Hoetelmans, Richard M W
AU - Iveson, Kathy J.
AU - Jayaweera, Dushyantha T
AU - Mills, Anthony M.
AU - Peeters, Monika P.
AU - Ruane, Peter J.
AU - Shalit, Peter
AU - Schrader, Shannon R.
AU - Smith, Stephen M.
AU - Steinhart, Corklin R.
AU - Thompson, Melanie
AU - Vingerhoets, Johan H.
AU - Voorspoels, Ellen
AU - Ward, Douglas
AU - Woodfall, Brian
PY - 2007/3/1
Y1 - 2007/3/1
N2 - OBJECTIVE: TMC125-C223 is an open-label, partially blinded, randomized clinical trial to evaluate the efficacy and safety of two dosages of etravirine (TMC125), a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against wild-type and NNRTI-resistant HIV-1. DESIGN: A total of 199 patients were randomly assigned 2:2:1 to twice-daily etravirine 400 mg, 800 mg and control groups, respectively. The primary endpoint was a change in viral load from baseline at week 24 in the intention-to-treat population. METHODS: Patients had HIV-1 with genotypic resistance to approved NNRTIs and at least three primary protease inhibitor (PI) mutations. Etravirine groups received an optimized background of at least two approved antiretroviral agents [nucleoside reverse transcriptase inhibitors (NRTI) and/or lopinavir/ritonavir and/or enfuvirtide]. Control patients received optimized regimens of at least three antiretroviral agents (NRTIs or PIs and/or enfuvirtide). RESULTS: The mean change from baseline in HIV-1 RNA at week 24 was -1.04, -1.18 and -0.19 log10 copies/ml for etravirine 400 mg twice a day, 800 mg twice a day and the control group, respectively (P < 0.05 for both etravirine groups versus control). Etravirine showed no dose-related effects on safety and tolerability. No consistent pattern of neuropsychiatric symptoms was observed. There were few hepatic adverse events, and rashes were predominantly early onset and mild to moderate in severity. CONCLUSION: Etravirine plus an optimized background significantly reduced HIV-1-RNA levels from baseline after 24 weeks in patients with substantial NNRTI and PI resistance, and demonstrated a favorable safety profile compared with control.
AB - OBJECTIVE: TMC125-C223 is an open-label, partially blinded, randomized clinical trial to evaluate the efficacy and safety of two dosages of etravirine (TMC125), a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against wild-type and NNRTI-resistant HIV-1. DESIGN: A total of 199 patients were randomly assigned 2:2:1 to twice-daily etravirine 400 mg, 800 mg and control groups, respectively. The primary endpoint was a change in viral load from baseline at week 24 in the intention-to-treat population. METHODS: Patients had HIV-1 with genotypic resistance to approved NNRTIs and at least three primary protease inhibitor (PI) mutations. Etravirine groups received an optimized background of at least two approved antiretroviral agents [nucleoside reverse transcriptase inhibitors (NRTI) and/or lopinavir/ritonavir and/or enfuvirtide]. Control patients received optimized regimens of at least three antiretroviral agents (NRTIs or PIs and/or enfuvirtide). RESULTS: The mean change from baseline in HIV-1 RNA at week 24 was -1.04, -1.18 and -0.19 log10 copies/ml for etravirine 400 mg twice a day, 800 mg twice a day and the control group, respectively (P < 0.05 for both etravirine groups versus control). Etravirine showed no dose-related effects on safety and tolerability. No consistent pattern of neuropsychiatric symptoms was observed. There were few hepatic adverse events, and rashes were predominantly early onset and mild to moderate in severity. CONCLUSION: Etravirine plus an optimized background significantly reduced HIV-1-RNA levels from baseline after 24 weeks in patients with substantial NNRTI and PI resistance, and demonstrated a favorable safety profile compared with control.
KW - 24-week primary analysis
KW - Etravirine
KW - Non-nucleoside reverse transcriptase inhibitor
KW - Randomized trial
KW - Resistant HIV-1
KW - TMC125
UR - http://www.scopus.com/inward/record.url?scp=34147134958&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=34147134958&partnerID=8YFLogxK
U2 - 10.1097/QAD.0b013e32805e8776
DO - 10.1097/QAD.0b013e32805e8776
M3 - Article
C2 - 17413684
AN - SCOPUS:34147134958
VL - 21
JO - AIDS
JF - AIDS
SN - 0269-9370
IS - 6
ER -