Table 4.
Advantages and Disadvantages of Currently Available Integrase Strand Transfer Inhibitors
| Dolutegravir | Elvitegravir | Raltegravir | |
|---|---|---|---|
| Year of US Food and Drug Administration approval |
2013 | 2012 | 2007 |
| Advantages | Superior to efavirenz and ritonavir-boosted darunavir in comparative clinical trials36,37 Once-daily dosing Coformulated with abacavir/lamivudine as part of a complete initial regimen Dolutegravir (not coformulated) pill size is small Lowest risk of resistance with virologic failure36,37,40,43 Relatively few drug interactions Can be taken with or without food Superior to raltegravir in treatment-experienced patients |
Superior to ritonavir-boosted atazanavir in comparative clinical trial in HIV-infected women38 Once-daily dosing Coformulated with tenofovir disoproxil fumarate/emtricitabine or tenofovir alafenamide/emtricitabine as a complete regimen |
Superior to ritonavir-boosted atazanavir and ritonavir-boosted darunavir in comparative clinical trial39 Longest safety record Fewest drug interactions Can be taken with or without food |
| Disadvantages | Only available coformulation is with abacavir/lamivudine Raises serum creatinine owing to inhibition of tubular secretion of creatinine Higher rates of insomnia and headache than comparators in some studies36,37 Largest tablet among coformulated single-pill regimens |
Requires pharmacokinetic boosting with cobicistat or ritonavir for once-daily dosing Most drug interactions Cobicistat raises serum creatinine owing to inhibition of tubular secretion of creatinine Should be taken with food |
Currently must be taken twice daily (formulation consisting of 2 pills given once daily in development) Not coformulated as part of a complete regimen |