| Combination INSTI + NNRTI |
| CAB plus RPV (PO or IM) | - This regimen only is approved for people who have achieved viral suppression on another ARV regimen. It has not been studied as initial ARV regimen.
|
| DTG plus RPV | - This regimen only is approved for people who have achieved viral suppression on another ARV regimen. It has not been studied as initial ARV regimen.
|
| NRTIs |
ABC/3TC/ZDV (Coformulated)
As triple-NRTI combination regimen | - Inferior virologic efficacy
|
ABC/3TC/ZDV plus TDF
As quadruple-NRTI combination regimen | - Inferior virologic efficacy
|
| d4T plus 3TC | - Significant toxicities (including lipoatrophy and peripheral neuropathy) and hyperlactatemia (including symptomatic and life-threatening lactic acidosis, hepatic steatosis, and pancreatitis)
|
| ddI plus 3TC (or FTC) | - Inferior virologic efficacy
- Limited clinical trial experience in ART-naive patients
- ddI toxicities, such as pancreatitis and peripheral neuropathy
|
| ddI plus TDF | - High rate of early virologic failure
- Rapid selection of resistance mutations
- Potential for immunologic nonresponse/CD4 cell decline
- Increased ddI drug exposure and toxicities
|
| ZDV/3TC | - Greater toxicities (including bone marrow suppression, GI toxicities, skeletal muscle myopathy, cardiomyopathy, and mitochondrial toxicities, such as lipoatrophy, lactic acidosis, and hepatic steatosis) than recommended NRTIs
|
| NNRTIs |
| DLV | - Inferior virologic efficacy
- Inconvenient (three times daily) dosing
|
| ETR | - Insufficient data in ART-naive patients
|
| NVP | - Associated with serious and potentially fatal toxicity (hepatic events and severe rash, including SJS and TEN)
- When compared to EFV, NVP did not meet noninferiority criteria
|
| PIs |
| ATV (Unboosted) | - Less potent than boosted ATV
|
| DRV (Unboosted) | - Use without RTV or COBI has not been studied
|
| FPV (Unboosted) or FPV/r | - Virologic failure with unboosted FPV-based regimen may result in selection of mutations that confer resistance to FPV and DRV
- Less clinical trial data for FPV/r than for other RTV-boosted PIs
|
| IDV (Unboosted) | - Inconvenient dosing (3 times daily with meal restrictions)/li>
- Fluid requirement
- IDV toxicities, such as nephrolithiasis and crystalluria
|
| IDV/r | - Fluid requirement
- IDV toxicities, such as nephrolithiasis and crystalluria
|
| LPV/r | - Higher pill burden than other PI-based regimens
- Higher RTV dose than other PI-based regimens
- GI intolerance
|
| NFV | - Inferior virologic efficacy
- Diarrhea
|
| RTV as sole PI | - High pill burden
- GI intolerance
- Metabolic toxicity
|
| SQV (Unboosted) | - Inadequate bioavailability
- Inferior virologic efficacy
|
| SQV/r | - High pill burden
- Can cause QT and PR prolongation; requires pretreatment and follow-up ECG
|
| TPV/r | - Inferior virologic efficacy
- Higher rate of adverse events than other RTV-boosted PIs
- Higher dose of RTV required for boosting than other RTV-boosted PIs
|
| Entry Inhibitors |
FTR
gp120 Attachment Inhibitor | - Only studied in a very small number of patients with virologic failure
|
IBA
CD4 Post-Attachment Inhibitor | - Only studied in a very small number of patients with virologic failure
- Requires IV therapy
- High cost
|
MVC
CCR5 Antagonist | - Requires testing for CCR5 tropism before initiation of therapy
- No virologic benefit when compared with other recommended regimens
- Requires twice-daily dosing
|
T20
Fusion Inhibitor | - Only studied in patients with virologic failure
- Twice-daily subcutaneous injections
- High rate of injection site reactions
|
| Key: 3TC = lamivudine; ABC = abacavir; ART = antiretroviral therapy; ARV = antiretroviral; ATV = atazanavir; CAB = cabotegravir; CD4 = CD4 T lymphocyte; COBI = cobicistat; d4T = stavudine; ddI = didanosine; DLV = delavirdine; DRV = darunavir; DTG = dolutegravir; ECG = electrocardiogram; EFV = efavirenz; ETR = etravirine; FPV = fosamprenavir; FPV/r = fosamprenavir/ritonavir; FTC = emtricitabine; FTR = fostemsavir; GI = gastrointestinal; IBA = ibalizumab; IDV = indinavir; IDV/r = indinavir/ritonavir; IM = intramuscular; IV = intravenous; LPV = lopinavir; LPV/r = lopinavir/ritonavir; MVC = maraviroc; NFV = nelfinavir; NNRTI = non-nucleoside reverse transcriptase inhibitor; NRTI = nucleoside reverse transcriptase inhibitor; NVP = nevirapine; PI = protease inhibitor; PO = oral; RPV = rilpivirine; RTV = ritonavir; SJS = Stevens Johnson Syndrome; SQV = saquinavir; SQV/r = saquinavir/ritonavir; T20 = enfuvirtide; TDF = tenofovir disoproxil fumarate; TEN = toxic epidermal necrolysis; TPV = tipranavir; TPV/r = tipranavir/ritonavir; ZDV = zidovudine |
