Table 1.
Atazanavir and ritonavir-boosted atazanavir efficacy studies.
| Study | Number and time (weeks) | Patient population | Atazanavir regimen (mg) | NNRTIs | Comparator regimen | Results | Ref. |
|---|---|---|---|---|---|---|---|
| AI424-007 | n = 420 48 |
ART-naive | 200 400 500 |
Didanosine Stavudine | NLF 750 mg t.i.d. | Viral and CD4 responses comparable across four arms resulted in unconjugated bilirubinemia in all arms and 12% in 500 mg arm. NLF resulted in 31% elevated lipids and 61% diarrhea | [30] |
| AI424-008 | n = 467 48 |
ART-naive | 400 600 |
Lamivudine Stavudine | NLF 1250 mg b.i.d. | Viral and CD4 responses comparable in all three arms. NLF resulted in 56% diarrhea and 33% decrease in those with desirable cholesterol levels | [31] |
| AI424-044 | n = 346 72 |
Roll over from AI424-008 | 400 600 |
Lamivudine Stavudine | Switch from NLF | Switch from NLF resulted in improved lipid profile and maintained viral suppression with long-term tolerability | [32] |
| AI424-034 | n = 810 48 |
ART-naive | 400 | Zidovudine Lamivudine | Efavirenz 600 mg once daily | Comparable efficacy of both arms. NB efavirenz virologic response somewhat lower than reported in prior studies | [33] |
| AI424-089 | n = 199 96 |
ART-naive | 400 | Lamivudine Stavudine-ER | RTV 300/100 mg once daily | ARV/RTV arm had nonstatistically significant trend for improved viral responses and significantly higher total cholesterol levels | [36] |
| COL103952 ‘ALERT’ | n = 94 48 |
ART-naive | RTV 300/100 | Tenofovir Emitricitabine | Fosamprenavir-APV/RTV 1400/100 mg once daily | Similar virological, CD4 cell count and lipid changes in both arms | [38] |
| Castle study | n = 878 48 |
ART-naive | RTV 300/100 | Tenofovir Emitricitabine | Tenofovir Emitricitabine | Ongoing 96-week study. Similar virologic and immunological outcomes. Diarrhea and lipid abnormalities lower in RTV arm | [39] |
| AI424-043 | n = 290 48 |
PI-experienced | 400 | Optimized background therapy | LPV/RTV 400/100 mg b.i.d. | LPV/RTV greater reduction in HIV RNA but increased lipids. RTV and LPV/RTV similar virologic responses in those without NRTI mutations at baseline | [34] |
| AI424-045 | n = 358 96 |
Failed two or more HAART regimens | RTV 300/100 | Tenofovir + one NRTI | SQV 400/1200 mg LPV/RTV 400/100 mg b.i.d. | SQV discontinued early by Data Safety Monitoring Board. RTV and LPV/RTV have similar virological efficacy. LPV/RTV associated with 9% increased cholesterol and 30% triglycerides and 13% grade 2–4 diarrhea. RTV associated with grade 3–4 bilirubin elevation in 53% | [40,41] |
APV: Amprenavir; ARV: Antiretroviral therapy; b.i.d.: Twice daily; ER: Extended release; HAART: Highly-active antiretroviral therapy; LPV: Lopinavir; NLF: Nelfinavir; NNRTI: Non-nucleoside reverse transcriptase inhibitor; NRTI: Nucleoside reverse transcriptase inhibitor; PI: Protease inhibitor; RTV: Ritonavir; SQV: Saquinavir; t.i.d.: Three-times daily.